CHO cells |
Function assay |
|
|
|
Ability to displace [3H]-SR- 141716A binding to human CB1 receptor expressed in CHO cell membranes, Ki=8.9 nM |
10465552 |
CHO |
Function assay |
|
|
|
Antagonistic activity towards cannabinoid receptor 1 expressed as [3H]Arachidonic acid release in CHO cells, Kd=0.002512μM |
14736243 |
CHO |
Function assay |
|
|
|
Displacement of CP-55940 binding from recombinant human cannabinoid receptor 1 expressed in CHO cells, Ki=0.025μM |
14736243 |
CHO |
Function assay |
|
|
|
Affinity to displace CP-55940 binding from Cannabinoid receptor 2 of human expressed in CHO cells, Ki=1.58μM |
14736243 |
CHO |
Function assay |
|
|
|
Inhibitory concentration against human recombinant cannabinoid receptor type 1 expressed in Chinese Hamster Ovary (CHO) cells, IC50=0.006μM |
15713403 |
CHO |
Function assay |
|
|
|
In vitro cannabinoid receptor 1 antagonism of [3H]arachidonic acid release by CHO cells, Kd=0.002512μM |
15771428 |
CHO |
Function assay |
|
|
|
In vitro displacement of CP-55940 binding to human CB1 receptor expressed in CHO cells, Ki=0.025μM |
15771428 |
CHO |
Function assay |
|
|
|
In vitro displacement of CP-55940 binding to human CB2 receptor expressed in CHO cells, Ki=1.58μM |
15771428 |
CHO |
Function assay |
|
|
|
Inhibition of [3H]SR-141,716A binding to human CB1 receptor expressed in CHO cells, Ki=0.0054μM |
15801840 |
CHO |
Function assay |
|
|
|
Antagonistic activity against cannabinoid receptor 1 measured by CP-55940 induced arachnoid acid release in CHO cells, Kd=0.002512μM |
16140010 |
CHO |
Function assay |
|
|
|
Displacement of specific CP-55940 binding in CHO cells stably transfected with human cannabinoid receptor 1, Ki=0.025μM |
16140010 |
CHO |
Function assay |
|
|
|
Displacement of specific CP-55940 binding in CHO cells stably transfected with human cannabinoid receptor 2, Ki=1.58μM |
16140010 |
CHOK1 |
Function assay |
|
|
|
Functional activity at human CB1 receptor transfected in CHOK1 cells by [35SGTP]gammaS assay, Ki=0.001μM |
16263283 |
HEK293 |
Function assay |
|
|
|
Displacement of [3H]SR-141716 from human CB1 receptor transfected in HEK293 cells, Ki=0.0021μM |
16263283 |
CHO |
Function assay |
|
|
|
Displacement of [3H]SR141716A from human CB1 receptor expressed in CHO cells, Ki=0.0054μM |
16279809 |
HEK293 |
Function assay |
|
|
|
Displacement of [3H]SR-141716 from human CB1 receptor expressed in HEK293 cells, Kd=0.0018μM |
17004712 |
HEK293 |
Function assay |
|
|
|
Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, Ki=0.0071μM |
17004712 |
HEK293 |
Function assay |
|
|
|
Displacement of [3H]WIN-55212-2 from human CB1 receptor expressed in HEK293 cells, Ki=0.018μM |
17004712 |
CHO |
Function assay |
|
|
|
Inhibition of [3H]CP-55940 binding to human recombinant CB1 receptor in CHO cells, IC50=0.0061μM |
17181138 |
CHO |
Function assay |
|
|
|
Inhibition of [3H]CP-55940 binding to human recombinant CB2 receptor in CHO cells, IC50=0.6μM |
17181138 |
CHO |
Function assay |
|
|
|
Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cells, IC50=0.0061μM |
17293109 |
CHO |
Function assay |
|
|
|
Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in CHO cells, IC50=0.6033μM |
17293109 |
HEK293 |
Function assay |
|
|
|
Displacement of [3H]CP-559440 from human CB1 receptor expressed in HEK293 cells, Ki=0.0011μM |
17383180 |
HEK293 |
Function assay |
|
|
|
Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells, Ki=0.016μM |
17942307 |
HEK293 |
Function assay |
|
|
|
Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells, Ki=1.64μM |
17942307 |
HEK293 |
Function assay |
|
|
|
Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells, Ki=0.047μM |
17979261 |
CHOK1 |
Function assay |
|
|
|
Displacement of [3H]WIN-552122 from human recombinant CB2 receptor expressed in CHOK1 cells, Ki=1.99μM |
17979261 |
HEK293 |
Function assay |
|
|
|
Displacement of radioligand from human CB1 receptor expressed in HEK293 cells, Ki=0.0018μM |
18083560 |
HEK293 EBNA |
Function assay |
|
|
|
Inverse agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgammaS incorporation assay, EC50=0.004μM |
18083560 |
HEK293 |
Function assay |
|
|
|
Displacement of radioligand from human CB2 receptor expressed in HEK293 cells, Ki=0.554μM |
18083560 |
CHOK1 |
Function assay |
|
|
|
Antagonist activity at human CB1 receptor expressed in CHOK1 cells by luciferase assay, IC50=0.12μM |
18243711 |
CHOK1 |
Function assay |
|
|
|
Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHOK1 cells, IC50=1.76μM |
18243711 |
HEK |
Function assay |
|
|
|
Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells, Ki=0.012μM |
18293908 |
HEK |
Function assay |
|
|
|
Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells, Ki=0.79μM |
18293908 |
HEK293 |
Function assay |
|
|
|
Displacement of [3H]CP-55940 from human CB1R expressed in HEK293 cells, Ki=0.006μM |
18335976 |
CHO |
Function assay |
|
|
|
Displacement of [3H]WIN-55212-2 from human cannabinoid CB2 receptor expressed in CHO cells, IC50=1.76μM |
18337096 |
CHO |
Function assay |
|
|
|
Displacement of [3H]CP-55940 from human CB1 receptor expressed in CHO cells, Ki=0.025μM |
18342403 |
CHO |
Function assay |
|
|
|
Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO cells, Ki=1.58μM |
18342403 |
HEK293 |
Function assay |
|
|
|
Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, Ki=0.0024μM |
18363352 |
CHO |
Function assay |
|
|
|
Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO cells, Ki=0.56μM |
18363352 |
SF9 |
Function assay |
|
|
|
Antagonist activity at rat CB1 receptor in SF9 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding, Ki=0.00031μM |
18448340 |
SF9 |
Function assay |
|
|
|
Antagonist activity at human CB1 receptor expressed in SF9 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding, Ki=0.00043μM |
18448340 |
SF9 |
Function assay |
|
|
|
Inverse agonist at human CB1 receptor expressed in SF9 cells assessed as decrease in GTPgammaS level, IC50=0.00135μM |
18448340 |
SF9 |
Function assay |
|
|
|
Antagonist activity at human CB2 receptor in SF9 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding, Ki=0.815μM |
18448340 |
HEK293 |
Function assay |
|
|
|
Displacement of [3H]CP-55940 form human recombinant CB1 receptor expressed in HEK293 cells by liquid scintillation counting, Ki=0.04μM |
18511157 |
CHO-K1 |
Function assay |
|
|
|
Displacement of [3H]SR141716 from human CB1 receptor expressed in CHO-K1 cells, Ki=0.00118μM |
18512901 |
HEK293 |
Function assay |
|
|
|
Antagonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of CP-55940-stimulated [35S]GTPgammaS binding, Kd=0.00257μM |
18512901 |
HEK293 |
Function assay |
|
|
|
Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, Ki=0.00618μM |
18512901 |
CHO-K1 |
Function assay |
|
|
|
Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO-K1 cells, Ki=0.313μM |
18512901 |
HEK |
Function assay |
|
|
|
Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells, Ki=0.008μM |
18579386 |
HEK |
Function assay |
|
|
|
Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells, Ki=0.79μM |
18579386 |
HEK293 |
Function assay |
|
|
|
Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, Ki=0.012μM |
18680276 |
HEK293 |
Function assay |
|
|
|
Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK293 cells, Ki=0.79μM |
18680276 |
HEK293 |
Function assay |
|
|
|
Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, IC50=0.015μM |
18712856 |
HEK293 |
Function assay |
|
|
|
Antagonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of Eu-GTP binding, EC50=0.0182μM |
18712856 |
HEK293 |
Function assay |
|
|
|
Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK293 cells, IC50=1.9398μM |
18712856 |
HEK293 |
Function assay |
|
|
|
Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as decrease in [35S]gammaGTP binding relative to control |
18712856 |
CHO |
Function assay |
|
|
|
Antagonist activity at human CB1 receptor in CHO cells assessed as GTPgammaS binding, Kb=0.000698μM |
18800770 |
CHOK1 |
Function assay |
|
|
|
Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHOK1 cells by liquid scintillation spectrometry, IC50=1.76μM |
18954042 |
CHO |
Function assay |
|
|
|
Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO cells, IC50=1.76μM |
19022666 |
HEK293 |
Function assay |
|
|
|
Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK293 cells, IC50=0.0019μM |
19095444 |
HEK293 |
Function assay |
|
|
|
Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, IC50=0.015μM |
19095444 |
HEK293 |
Function assay |
|
|
|
Antagonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of Eu-GTP binding, EC50=0.0182μM |
19095444 |
CHO-K1 |
Function assay |
|
|
|
Antagonist activity against human CB1 receptor expressed in CHO-K1 cells by [35S]GTPgamma binding assay, Ki=0.00019μM |
19102698 |
HEK293 |
Function assay |
|
|
|
Displacement of [3H]SR141716A from human CB1 receptor expressed in HEK293 cells, Ki=0.0009μM |
19102698 |
CHOK1 |
Function assay |
|
|
|
Displacement of [3H]WIN-55212-2 from human recombinant cannabinoid CB2 receptor expressed in CHOK1 cells by liquid scintillation spectrometry, IC50=1.76μM |
19269817 |
CHOK1 |
Function assay |
|
|
|
Antagonist activity at human cannabinoid CB1 receptor expressed in CHOK1 cells assessed as cAMP activity, EC50=0.24μM |
19328683 |
CHOK1 |
Function assay |
|
|
|
Antagonist activity at human cannabinoid CB2 receptor expressed in CHOK1 cells assessed as cAMP activity, EC50=31.21μM |
19328683 |
HEK293 |
Function assay |
|
|
|
Displacement of [3H]SR141716 from human recombinant CB1 receptor expressed in HEK293 cells, Ki=0.001995μM |
19338356 |
HEK293 |
Function assay |
|
|
|
Displacement of [3H]SR141716 from human recombinant CB2 receptor expressed in HEK293 cells, Ki=0.39811μM |
19338356 |
CHOK1 |
Function assay |
|
10 mins |
|
Antagonist activity at human CB1 receptor expressed in CHOK1 cells assessed as inhibition of CP-55940-induced response after 10 mins by GTPgamma[35S] binding assay, Ki=0.0016μM |
19351113 |
HEK293 |
Function assay |
|
|
|
Displacement of [3H]rimonabant from human CB1 receptor expressed in HEK293 cells by liquid scintillation counting, Ki=0.0019μM |
19520572 |
HEK293 |
Function assay |
|
|
|
Displacement of [3H]CP-55940 from human recombinant CB1R expressed in HEK293 cells, IC50=0.0132μM |
19530697 |
HEK293 |
Function assay |
|
|
|
Inverse agonist activity at human recombinant CB1R expressed in HEK293 cells assessed as inhibition of CP-55940-stimulated Eu-GTP binding, EC50=0.0157μM |
19530697 |
HEK293 |
Function assay |
|
|
|
Displacement of [3H]CP-55940 from human recombinant CB2R expressed in HEK293 cells, IC50=1.6311μM |
19530697 |
HEK293 |
Function assay |
10 uM |
|
|
Intrinsic activity at human recombinant CB1R expressed in HEK293 cells assessed as Eu-GTP binding at 10 uM relative to basal level |
19530697 |
HEK |
Function assay |
|
|
|
Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells, Ki=0.012μM |
19595596 |
HEK |
Function assay |
|
|
|
Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells, Ki=0.79μM |
19595596 |
CHO-K1 |
Function assay |
|
|
|
Antagonist activity at human CB1 receptor transfected in CHO-K1cells by GTPgamma[35S] binding assay, Ki=0.0016μM |
19683918 |
CHO |
Function assay |
|
|
|
Binding affinity to human CB2 receptor expressed in CHO cells by luciferase reporter gene assay, IC50=0.0925μM |
19850473 |
CHOK1 |
Function assay |
|
|
|
Displacement of [3H]WIN-552122 from human CB2 receptor expressed in CHOK1 cells, IC50=1.76μM |
19850473 |
CHO-K1 |
Function assay |
|
|
|
Antagonist activity at human recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding, IC50=0.0045μM |
19954978 |
CHO-K1 |
Function assay |
|
|
|
Inverse agonist activity at human CB1 receptor expressed in CHO-K1 cells by GTPgammaS binding assay, IC50=0.0029μM |
20015647 |
CHO-K1 |
Function assay |
|
|
|
Antagonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP-55940-induced GTPgammaS binding, IC50=0.0045μM |
20015647 |
COS7 |
Function assay |
|
|
|
Displacement of [3H]CP-55940 from human CB1 receptor expressed in COS7 cells, IC50=0.0051μM |
20015647 |
CHO |
Function assay |
|
|
|
Inverse agonist activity at human recombinant CB1 receptor expressed in CHO cells by luciferase reporter gene assay, IC50=0.108μM |
20045337 |
CHO |
Function assay |
|
60 mins |
|
Inverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 mins, EC50=0.00011μM |
20047779 |
CHO |
Function assay |
|
3 hrs |
|
Displacement of [3H]CP-55940 from human recombinant cannabinoid CB1 receptor expressed in CHO cells after 3 hrs by liquid scintillation counting, Ki=0.00074μM |
20047779 |
CHO |
Function assay |
|
10 mins |
|
Antagonist activity at human cannabinoid CB1 receptor expressed in CHO cells coexpressing Galpha15/16 assessed as inhibition of CP-55940-induced Ca2+ release after 10 mins by micro plate reader, IC50=0.0032μM |
20047779 |
CHO |
Function assay |
|
3 hrs |
|
Displacement of [3H]CP-55940 from human recombinant cannabinoid CB2 receptor expressed in CHO cells after 3 hrs by liquid scintillation counting, Ki=0.126μM |
20047779 |
CHO |
Function assay |
|
|
|
Antagonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of CP-55940-induced [3H]arachidonic acid release, Kd=0.002512μM |
20363132 |
CHO |
Function assay |
|
|
|
Displacement of [3H]CP-55940 from human CB1 receptor expressed in CHO cells, Ki=0.025μM |
20363132 |
CHO |
Function assay |
|
|
|
Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO cells, Ki=1.58μM |
20363132 |
CHO-K1 |
Function assay |
|
1 hr |
|
Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation counting, IC50=1.76μM |
20673729 |
HEK |
Function assay |
|
|
|
Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK cells, Ki=0.012μM |
20718492 |
HEK |
Function assay |
|
|
|
Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK cells, Ki=0.79μM |
20718492 |
CHO |
Function assay |
|
|
|
Agonist activity at human CB1 receptor expressed in CHO cells co-expressing Galpha16 protein assessed as mobilization of intracellular calcium, Ke=0.0011μM |
20845959 |
HEK293 |
Function assay |
|
|
|
Displacement of [3H]SR141716 from human CB1 receptor expressed in HEK293 cells, Ki=0.00118μM |
20845959 |
HEK293 |
Function assay |
|
|
|
Displacement of [3H]CP55940 from human CB1 receptor expressed in HEK293 cells, Ki=0.00618μM |
20845959 |
CHOK1 |
Function assay |
|
|
|
Displacement of [3H]CP55940 from human CB2 receptor expressed in CHOK1 cells, Ki=0.313μM |
20845959 |
HEK |
Function assay |
|
|
|
Displacement of [3H]CP-55,940 from recombinant human CB1 receptor transfected in HEK cells, Ki=0.012μM |
20943290 |
HEK |
Function assay |
|
|
|
Displacement of [3H]CP-55,940 from recombinant human CB2 receptor transfected in HEK cells, Ki=0.79μM |
20943290 |
CHO |
Function assay |
|
|
|
Displacement of [3H]SR141716A from human CB1 receptor expressed in CHO cells, Ki=0.0009333μM |
21334892 |
Sf9 |
Function assay |
|
|
|
Displacement of [3H]CP55940 from human recombinant CB2 receptor expressed in Sf9 cells, Ki=0.85114μM |
21334892 |
CHO |
Function assay |
|
|
|
Antagonist activity at CB1 receptor transfected in CHO cells expressing apoaequorin as a reporter for G-protein-coupled receptor-mediated calcium signaling by bioluminescence assay, IC50=0.004μM |
21376588 |
HEK293 |
Function assay |
|
|
|
Noncompetitive inhibition of MRP1-mediated E2-17betaG transport in human MRP1 expressing HEK293 cells by Dixon plot, Ki=1.4μM |
21511945 |
HEK293 |
Function assay |
|
|
|
Noncompetitive inhibition of MRP4-mediated E2-17betaG transport in human MRP4 expressing HEK293 cells by Dixon plot, Ki=4μM |
21511945 |
HEK293 |
Function assay |
|
|
|
Induction of MRP2-mediated E2-17betaG transport in human MRP2 expressing HEK293 cells in presence of 2 uM E2-17betaG |
21511945 |
HEK293 |
Function assay |
|
|
|
Inhibition of MRP3-mediated E2-17betaG transport in human MRP3 expressing HEK293 cells in presence of 15 uM E2-17betaG |
21511945 |
HEK293 |
Function assay |
|
|
|
Inhibition of MRP1-mediated E2-17betaG transport in human MRP1 expressing HEK293 cells in presence of 0.6 to 5 uM E2-17betaG |
21511945 |
HEK293 |
Function assay |
|
|
|
Inhibition of MRP4-mediated E2-17betaG transport in human MRP4 expressing HEK293 cells in presence of 0.6 to 5 uM E2-17betaG |
21511945 |
HEK |
Function assay |
|
|
|
Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells, Ki=0.012μM |
21702498 |
HEK |
Function assay |
|
|
|
Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells, Ki=0.79μM |
21702498 |
CHO |
Function assay |
|
1 hr |
|
Displacement of [3H]CP55940 from human cannabinoid CB2 receptor expressed in CHO cells at pH 7.4 after 1 hr by liquid scintillation counting, IC50=1.98μM |
21741835 |
HEK293 |
Function assay |
|
5 mins |
|
Inhibition of human ERG expressed in HEK293 cells assessed as inhibition of potassium channel current after 5 mins by patch clamp assay, IC50=2.79μM |
21741835 |
CHO |
Function assay |
|
90 mins |
|
Displacement of [3H]BMS-725519 from human CB1 receptor expressed in CHO cells after 90 mins by scintillation counting, Ki=0.00073μM |
21962575 |
CHO-K1 |
Function assay |
|
|
|
Antagonist activity at human CB1 receptor expressed in CHO-K1 cells co-expressing Galphaq16 assessed as inhibition of CP55940-induced intracellular calcium mobilization by fluorometry, Ke=0.0011μM |
22372835 |
CHO-K1 |
Function assay |
|
|
|
Displacement of [3H]CP55940 from human CB1 receptor expressed in CHO-K1 cells, Ki=0.0062μM |
22372835 |
CHO-K1 |
Function assay |
|
|
|
Displacement of [3H]CP55940 from CB2 receptor expressed in CHO-K1 cells, Ki=0.313μM |
22372835 |
HEK |
Function assay |
|
|
|
Displacement of [3H]CP-55,940 from human recombinant CB1 receptor transfected in HEK cells, Ki=0.012μM |
22548457 |
HEK |
Function assay |
|
|
|
Displacement of [3H]CP-55,940 from human recombinant CB2 receptor transfected in HEK cells, Ki=0.79μM |
22548457 |
CHO |
Function assay |
|
2 hrs |
|
Displacement of [3H]CP55,940 from human CB1 receptor expressed in CHO cells after 2 hrs by liquid scintillation counter, Ki=0.0126μM |
22916707 |
CHO |
Function assay |
|
2 hrs |
|
Displacement of [3H]CP55,940 from human CB2 receptor expressed in CHO cells after 2 hrs by liquid scintillation counter, Ki=0.9μM |
22916707 |
CHO |
Function assay |
|
|
|
Inverse agonist activity against CB1 receptor expressed in human CHO cells assessed as effect on forskolin-stimulated cAMP level, IC50=0.051μM |
22959249 |
CHO |
Function assay |
|
1 hr |
|
Displacement of [3H]CP55940 from human CB1 receptor expressed in CHO cells incubated for 1 hr, Ki=0.0106μM |
23072339 |
CHO |
Function assay |
> 0.1 nM |
1 hr |
|
Inverse agonist activity at human recombinant CB1 receptor transfected in CHO cells assessed as reduction of [35S]GTPgammaS binding at > 0.1 nM after 1 hr by liquid scintillation spectrometry |
23357307 |
N1E-115 |
Function assay |
1 uM |
5 mins |
|
Inverse agonist activity at CB1 receptor in mouse N1E-115 cells assessed as inhibition of WIN 55,212-2-induced ERK1/2 phosphorylation at 1 uM treated 5 mins prior to WIN 55,212-2 challenge by Western blot analysis |
23357307 |
CHO |
Function assay |
|
|
|
Antagonist activity at human GPR18 transfected in CHO cells assessed as delta9-THC-induced beta-arrestin recruitment incubated 60 mins prior to delta9-THC addition by beta-arrestin translocation assay, IC50=10.1μM |
23679955 |
HEK |
Function assay |
|
1 hr |
|
Antagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysis, EC50=0.0015μM |
24175572 |
CHOK1 |
Function assay |
|
1 hr |
|
Displacement of [3H]CP55940 from human CB1 receptor expressed in CHOK1 cells after 1 hr by liquid scintillation counting analysis, Ki=0.0059μM |
24175572 |
CHO |
Function assay |
|
45 mins |
|
Antagonist activity at human CB1 receptor stably expressed in CHO cells co-expressing co-expressing Ga15/16 assessed as calcium current after 45 mins by fluo-4 AM assay, IC50=0.013μM |
24445310 |
CHO |
Function assay |
|
45 mins |
|
Antagonist activity at CB2 receptor (unknown origin) stably expressed in CHO cells co-expressing co-expressing Ga15/16 assessed as calcium current after 45 mins by fluo-4 AM assay, IC50=9.8μM |
24445310 |
CHO-K1 |
Function assay |
|
10 mins |
|
Antagonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP-55940-induced [35S]GTPgammaS binding incubated for 10 mins prior to CP-55940-challenge measured after 1 hr by beta counting, Ki=0.0016μM |
24900484 |
HEK293 |
Function assay |
|
60 mins |
|
Displacement of [3H]SR141716A form human CB1 receptor expressed in HEK293 cells after 60 mins by beta counting, Ki=0.0018μM |
24900484 |
CHO-K1 |
Function assay |
|
60 mins |
|
Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO-K1 cells after 60 mins by beta counting, Ki=0.522μM |
24900484 |
CHO |
Function assay |
|
2 hrs |
|
Displacement of [3H]CP55,940 from recombinant human CB1 receptor expressed in CHO cells after 2 hrs by liquid scintillation counting, Ki=0.0126μM |
24900561 |
CHO |
Function assay |
|
2 hrs |
|
Displacement of [3H]CP55,940 from recombinant human CB2 receptor expressed in CHO cells after 2 hrs by liquid scintillation counting, Ki=0.9μM |
24900561 |
CHO |
Function assay |
|
90 mins |
|
Agonist activity at GPR55 (unknown origin) expressed in CHO cells assessed as inhibition of LPI-induced beta-arrestin translocation after 90 mins by luminescence assay, EC50=2.01μM |
24900561 |
RD-HGA16 |
Function assay |
|
|
|
Antagonist activity at CB1-OX1 heterodimer (unknown origin) expressed in RD-HGA16 cells assessed as inhibition of orexin A-induced calcium mobilization by fluorometric imaging plate reader analysis, Ke=0.001μM |
24944734 |
RD-HGA16 |
Function assay |
|
|
|
Antagonist activity at CB1 receptor (unknown origin) expressed in RD-HGA16 cells assessed as inhibition of CP55940-induced calcium mobilization by fluorometric imaging plate reader analysis, Ke=0.0011μM |
24944734 |
Sf9 |
Function assay |
|
20 mins |
|
Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay, EC50=0.05μM |
25096297 |
Sf9 |
Function assay |
|
20 mins |
|
Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay, EC50=0.05012μM |
25096297 |
CHO |
Function assay |
|
|
|
Antagonist activity against CB1R (unknown origin) CHO cells stably expressing Galpha16 assessed as inhibition of CP55940-induced increase in intracellular calcium level pre-treated 10 mins before CP55940 stimulation by microplate reader based assay, IC50=0.0135μM |
26151231 |
CHO |
Function assay |
|
|
|
Antagonist activity against CB2R (unknown origin) CHO cells stably expressing Galpha16 assessed as inhibition of CP55940-induced increase in intracellular calcium level pre-treated 10 mins before CP55940 stimulation by microplate reader based assay, IC50=9.1μM |
26151231 |
HEK293 |
Function assay |
|
|
|
Immediate antagonist/Inverse agonist activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as reversal of 1 uM CP55,940-induced inhibition of 5 uM forskolin-induced cAMP accumulation by kinetic cAMP assay |
26203658 |
HEK293 |
Function assay |
|
90 mins |
|
Displacement of [3H]-CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells after 90 mins by Competition binding assay, Kieq=0.012μM |
26756097 |
HEK293 |
Function assay |
|
90 mins |
|
Displacement of [3H]-CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells after 90 mins by Competition binding assay, Kieq=0.79μM |
26756097 |
CHO-K1 |
Function assay |
|
|
|
Antagonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP55940-induced intracellular calcium mobilization by Calcein-4 AM-staining based FLIPR assay, Ke=0.0011μM |
26827137 |
CHO |
Function assay |
|
90 secs |
|
Inverse agonist activity at human CB1 receptor expressed in CHO cells assessed as increase in intracellular calcium mobilization after 90 secs by Calcein-4 AM-staining based FLIPR assay, EC50=0.005μM |
26827137 |
SJ-GBM2 |
qHTS assay |
|
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells |
29435139 |
A673 |
qHTS assay |
|
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells |
29435139 |
SK-N-MC |
qHTS assay |
|
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells |
29435139 |
BT-37 |
qHTS assay |
|
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells |
29435139 |
SK-N-SH |
qHTS assay |
|
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells |
29435139 |
NB1643 |
qHTS assay |
|
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells |
29435139 |
LAN-5 |
qHTS assay |
|
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells |
29435139 |
BT-12 |
qHTS assay |
|
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells |
29435139 |
OHS-50 |
qHTS assay |
|
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells |
29435139 |
RD |
qHTS assay |
|
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells |
29435139 |
A673 |
qHTS assay |
|
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) |
29435139 |
SK-N-MC |
qHTS assay |
|
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells |
29435139 |
DAOY |
qHTS assay |
|
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells |
29435139 |
TC32 |
qHTS assay |
|
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells |
29435139 |
U-2 OS |
qHTS assay |
|
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells |
29435139 |
Rh41 |
qHTS assay |
|
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells |
29435139 |
Saos-2 |
qHTS assay |
|
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells |
29435139 |
CHOK1 |
Function assay |
|
90 mins |
|
Inverse agonist activity at C-terminally prolink-tagged mouse CB2 receptor expressed in CHOK1 cells harboring beta-galactosidase enzyme fused beta-arrestin assessed as increase in beta-arrestin recruitment after 90 mins by chemiluminescent assay, EC50=0.015μM |
29939744 |
HEK293 |
Function assay |
|
|
|
Antagonist activity at human CB1 receptor expressed in HEK293 cells by GTPgammaS binding assay, Ke=0.0002μM |
30077609 |
HEK293 |
Function assay |
|
90 secs |
|
Inverse agonist activity at human CB1 receptor expressed in HEK293 cells co-expressing Galphaq16 assessed as inhibition of calcium mobilization after 90 secs by calcein-4 AAM dye-based FLIPR assay, EC50=0.586μM |
30077609 |
HEK293 |
Function assay |
|
30 mins |
|
Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay, EC50=0.0041μM |
30339387 |
CHO |
Function assay |
|
|
|
Displacement of [3H]-CP55940 from human recombinant cannabinoid CB1 receptor expressed in CHO cells by radioligand binding assay, Ki=0.143μM |
31609608 |
CHO |
Function assay |
|
|
|
Agonist activity at human GPR55 expressed in CHO cells assessed as induction of LPI-induced beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method, EC50=2.01μM |
ChEMBL |
CHO |
Function assay |
|
|
|
Agonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method, EC50=10.1μM |
ChEMBL |