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Assay Detail

CHEMBL1040518

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

Functional
Agonist activity at canine TGR5 expressed in melanophores assessed as melanosome dispersion by melanophore assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Canis lupus familiaris
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of 3-aryl-4-isoxazolecarboxamides as TGR5 receptor agonists.
Evans KA, Budzik BW, Ross SA, Wisnoski DD, Jin J, Rivero RA, Vimal M, Szewczyk GR, Jayawickreme C, Moncol DL, Rimele TJ, Armour SL, Weaver SP, Griffin RJ, Tadepalli SM, Jeune MR, Shearer TW, Chen ZB, Chen L, Anderson DL, Becherer JD, De Los Frailes M, Colilla FJ.
J Med Chem (2009) 52 : 7962 -7965
PubMed 19902954 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 7.35 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL576138 1 7.50
CHEMBL575966 1 7.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL576138 EC50 = 31.62 nM 7.50
CHEMBL575966 EC50 = 63.1 nM 7.20