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Assay Detail

CHEMBL693096

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Functional
Dissociation constant [100(nM)] in myenteric plexus-longitudinal muscle of guinea pig small intestine using the cannabinoid receptor agonist.
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Small intestine
Confidence 1 — Organism
Curated By Intermediate

Target

Cavia porcellus (CHEMBL369)
Type ORGANISM
Organism Cavia porcellus

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
Kd 5 9.06 9.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL285932 1 9.66
CHEMBL111 RIMONABANT 4.0 1 9.60
CHEMBL286188 1 9.49
CHEMBL349955 1 8.58
CHEMBL424527 1 7.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL285932 Kd = 0.22 nM 9.66
CHEMBL111 RIMONABANT Kd = 0.25 nM 9.60
CHEMBL286188 Kd = 0.32 nM 9.49
CHEMBL349955 Kd = 2.63 nM 8.58
CHEMBL424527 Kd = 11.2 nM 7.95