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Assay Detail

CHEMBL901386

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Functional
Agonist activity at GHSR
4
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Growth hormone secretagogue receptor type 1 (CHEMBL4616)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, in vitro, and in vivo characterization of phenylpiperazines and pyridinylpiperazines as potent and selective antagonists of the melanocortin-4 receptor.
Tran JA, Jiang W, Tucci FC, Fleck BA, Wen J, Sai Y, Madan A, Chen TK, Markison S, Foster AC, Hoare SR, Marks D, Harman J, Chen CW, Arellano M, Marinkovic D, Bozigian H, Saunders J, Chen C.
J Med Chem (2007) 50 : 6356 -6366
PubMed 17994683 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 6.62 7.10
Intrinsic activity 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL393576 2 7.10
CHEMBL266647 2 6.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL393576 EC50 = 79.0 nM 7.10
CHEMBL266647 EC50 = 720.0 nM 6.14
CHEMBL266647 Intrinsic activity = 47.0 % -
CHEMBL393576 Intrinsic activity = 107.0 % -