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Assay Detail

CHEMBL657998

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

Binding
Binding affinity against Cannabinoid receptor 2 in mouse spleen
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cannabinoid receptor 2 (CHEMBL5373)
Type SINGLE PROTEIN
Organism Mus musculus

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 6.11 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL285486 1 8.72
CHEMBL36569 1 6.67
CHEMBL285153 1 6.66
CHEMBL349512 1 6.60
CHEMBL165134 1 6.24
CHEMBL349513 1 6.16
CHEMBL354476 1 6.13
CHEMBL36250 1 6.08
CHEMBL424527 1 6.03
CHEMBL349955 1 6.02
CHEMBL34201 1 6.00
CHEMBL285473 1 5.90
CHEMBL167661 1 5.88
CHEMBL286188 1 5.84
CHEMBL111 RIMONABANT 4.0 1 5.79
CHEMBL285932 1 5.64
CHEMBL422034 1 5.63
CHEMBL33652 1 5.61
CHEMBL352460 1 5.34
CHEMBL35657 1 5.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL285486 Ki = 1.9 nM 8.72
CHEMBL36569 Ki = 215.0 nM 6.67
CHEMBL285153 Ki = 217.0 nM 6.66
CHEMBL349512 Ki = 252.0 nM 6.60
CHEMBL165134 Ki = 577.0 nM 6.24
CHEMBL349513 Ki = 691.0 nM 6.16
CHEMBL354476 Ki = 744.0 nM 6.13
CHEMBL36250 Ki = 836.0 nM 6.08
CHEMBL424527 Ki = 931.0 nM 6.03
CHEMBL349955 Ki = 958.0 nM 6.02
CHEMBL34201 Ki = 1010.0 nM 6.00
CHEMBL285473 Ki = 1260.0 nM 5.90
CHEMBL167661 Ki = 1310.0 nM 5.88
CHEMBL286188 Ki = 1430.0 nM 5.84
CHEMBL111 RIMONABANT Ki = 1640.0 nM 5.79
CHEMBL285932 Ki = 2290.0 nM 5.64
CHEMBL422034 Ki = 2340.0 nM 5.63
CHEMBL33652 Ki = 2450.0 nM 5.61
CHEMBL352460 Ki = 4580.0 nM 5.34
CHEMBL35657 Ki = 6750.0 nM 5.17