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Assay Detail

CHEMBL4236333

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Functional
Agonist activity at recombinant rat Cb1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP levels
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Oximes short-acting CB1 receptor agonists.
Malamas MS, Raghav JG, Ma X, Honrao C, Wood JT, Benchama O, Zhou H, Mallipeddi S, Makriyannis A.
Bioorg Med Chem (2018) 26 : 4963 -4970
PubMed 30122284 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 8.65 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4240671 1 9.40
CHEMBL4240996 1 9.24
CHEMBL4242964 1 9.15
CHEMBL4249729 1 9.05
CHEMBL4237501 1 8.59
CHEMBL559612 CP-55940 1 8.52
CHEMBL4249273 1 8.36
CHEMBL4243768 1 7.90
CHEMBL4244186 1 7.65
CHEMBL4239190 1 -
CHEMBL4245472 1 -
CHEMBL4238778 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4240671 EC50 = 0.4 nM 9.40
CHEMBL4240996 EC50 = 0.58 nM 9.24
CHEMBL4242964 EC50 = 0.7 nM 9.15
CHEMBL4249729 EC50 = 0.9 nM 9.05
CHEMBL4237501 EC50 = 2.6 nM 8.59
CHEMBL559612 CP-55940 EC50 = 3.0 nM 8.52
CHEMBL4249273 EC50 = 4.4 nM 8.36
CHEMBL4243768 EC50 = 12.7 nM 7.90
CHEMBL4244186 EC50 = 22.4 nM 7.65
CHEMBL4239190 EC50 - -
CHEMBL4245472 EC50 - -
CHEMBL4238778 EC50 - -