Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL658897

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

Binding
Binding affinity against Cannabinoid receptor 1 in rat forebrain
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists.
Lan R, Liu Q, Fan P, Lin S, Fernando SR, McCallion D, Pertwee R, Makriyannis A.
J Med Chem (1999) 42 : 769 -776
PubMed 10052983 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 7.22 8.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL285932 1 8.13
CHEMBL36569 1 8.11
CHEMBL111 RIMONABANT 4.0 1 7.94
CHEMBL34201 1 7.93
CHEMBL286188 1 7.78
CHEMBL167661 1 7.77
CHEMBL35657 1 7.51
CHEMBL33652 1 7.27
CHEMBL165134 1 7.27
CHEMBL349512 1 7.24
CHEMBL36250 1 7.22
CHEMBL285473 1 7.12
CHEMBL349955 1 7.09
CHEMBL285153 1 6.91
CHEMBL352460 1 6.90
CHEMBL354476 1 6.74
CHEMBL349513 1 6.59
CHEMBL422034 1 6.49
CHEMBL424527 1 6.46
CHEMBL285486 1 5.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL285932 Ki = 7.49 nM 8.13
CHEMBL36569 Ki = 7.85 nM 8.11
CHEMBL111 RIMONABANT Ki = 11.5 nM 7.94
CHEMBL34201 Ki = 11.7 nM 7.93
CHEMBL286188 Ki = 16.8 nM 7.78
CHEMBL167661 Ki = 17.1 nM 7.77
CHEMBL35657 Ki = 31.1 nM 7.51
CHEMBL33652 Ki = 53.9 nM 7.27
CHEMBL165134 Ki = 53.8 nM 7.27
CHEMBL349512 Ki = 57.5 nM 7.24
CHEMBL36250 Ki = 60.4 nM 7.22
CHEMBL285473 Ki = 76.7 nM 7.12
CHEMBL349955 Ki = 81.5 nM 7.09
CHEMBL285153 Ki = 123.0 nM 6.91
CHEMBL352460 Ki = 125.0 nM 6.90
CHEMBL354476 Ki = 183.0 nM 6.74
CHEMBL349513 Ki = 255.0 nM 6.59
CHEMBL422034 Ki = 326.0 nM 6.49
CHEMBL424527 Ki = 346.0 nM 6.46
CHEMBL285486 Ki = 1120.0 nM 5.95