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Assay Detail

CHEMBL864630

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Displacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptor
48
Total Activities
24
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Cannabinoid receptor 1 (CHEMBL3571)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

3D-QSAR studies on cannabinoid CB1 receptor agonists: G-protein activation as biological data.
Salo OM, Savinainen JR, Parkkari T, Nevalainen T, Lahtela-Kakkonen M, Gynther J, Laitinen JT, Järvinen T, Poso A.
J Med Chem (2006) 49 : 554 -566
PubMed 16420041 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 24 5.73 8.30
Emax 24 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL307696 2 8.30
CHEMBL336670 2 8.00
CHEMBL199561 2 8.00
CHEMBL559612 CP-55940 2 7.00
CHEMBL465 DRONABINOL 4.0 2 6.70
CHEMBL74415 CANNABINOL 3.0 2 6.50
CHEMBL151167 2 6.50
CHEMBL418353 2 6.40
CHEMBL267227 DELTA-8-TETRAHYDROCANNABINOL 2.0 2 6.20
CHEMBL201758 2 5.90
CHEMBL371214 2 5.70
CHEMBL380923 2 5.70
CHEMBL199911 2 5.50
CHEMBL201260 2 5.50
CHEMBL150849 2 5.10
CHEMBL15848 ANANDAMIDE 2 4.80
CHEMBL203474 2 4.80
CHEMBL113473 2 4.60
CHEMBL281211 ARACHIDONYL TRIFLUOROMETHYLKETONE 2 4.60
CHEMBL200113 2 4.40
CHEMBL320549 2 4.40
CHEMBL371953 2 4.30
CHEMBL199668 2 4.30
CHEMBL381893 2 4.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL307696 EC50 = 5.012 nM 8.30
CHEMBL199561 EC50 = 10.0 nM 8.00
CHEMBL336670 EC50 = 10.0 nM 8.00
CHEMBL559612 CP-55940 EC50 = 100.0 nM 7.00
CHEMBL465 DRONABINOL EC50 = 199.53 nM 6.70
CHEMBL151167 EC50 = 316.23 nM 6.50
CHEMBL74415 CANNABINOL EC50 = 316.23 nM 6.50
CHEMBL418353 EC50 = 398.11 nM 6.40
CHEMBL267227 DELTA-8-TETRAHYDROCANNABINOL EC50 = 630.96 nM 6.20
CHEMBL201758 EC50 = 1258.93 nM 5.90
CHEMBL380923 EC50 = 1995.26 nM 5.70
CHEMBL371214 EC50 = 1995.26 nM 5.70
CHEMBL201260 EC50 = 3162.28 nM 5.50
CHEMBL199911 EC50 = 3162.28 nM 5.50
CHEMBL150849 EC50 = 7943.28 nM 5.10
CHEMBL15848 ANANDAMIDE EC50 = 15848.93 nM 4.80
CHEMBL203474 EC50 = 15848.93 nM 4.80
CHEMBL113473 EC50 = 25118.86 nM 4.60
CHEMBL281211 ARACHIDONYL TRIFLUOROMETHYLKETONE EC50 = 25118.86 nM 4.60
CHEMBL320549 EC50 = 39810.72 nM 4.40
CHEMBL200113 EC50 = 39810.72 nM 4.40
CHEMBL381893 EC50 = 50118.72 nM 4.30
CHEMBL199668 EC50 = 50118.72 nM 4.30
CHEMBL371953 EC50 = 50118.72 nM 4.30
CHEMBL199668 Emax = 382.0 % -
CHEMBL465 DRONABINOL Emax = 159.0 % -
CHEMBL201260 Emax = 199.0 % -
CHEMBL381893 Emax = 474.0 % -
CHEMBL199911 Emax = 213.0 % -
CHEMBL371214 Emax = 158.0 % -
CHEMBL74415 CANNABINOL Emax = 131.0 % -
CHEMBL199561 Emax = 400.0 % -
CHEMBL336670 Emax = 369.0 % -
CHEMBL307696 Emax = 396.0 % -
CHEMBL559612 CP-55940 Emax = 443.0 % -
CHEMBL267227 DELTA-8-TETRAHYDROCANNABINOL Emax = 184.0 % -
CHEMBL371953 Emax = 332.0 % -
CHEMBL200113 Emax = 352.0 % -
CHEMBL151167 Emax = 326.0 % -
CHEMBL203474 Emax = 284.0 % -
CHEMBL320549 Emax = 269.0 % -
CHEMBL150849 Emax = 286.0 % -
CHEMBL15848 ANANDAMIDE Emax = 380.0 % -
CHEMBL113473 Emax = 255.0 % -
CHEMBL380923 Emax = 260.0 % -
CHEMBL201758 Emax = 210.0 % -
CHEMBL281211 ARACHIDONYL TRIFLUOROMETHYLKETONE Emax = 161.0 % -
CHEMBL418353 Emax = 351.0 % -