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Assay Detail

CHEMBL854909

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

Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
10
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type IMR-32
Confidence 9 — Direct single protein target
Curated By Expert

Target

Melanin-concentrating hormone receptor 1 (CHEMBL344)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Constrained 7-fluorocarboxychromone-4-aminopiperidine based Melanin-concentrating hormone receptor 1 antagonists: the effects of chirality on substituted indan-1-ylamines.
Souers AJ, Iyengar RR, Judd AS, Beno DW, Gao J, Zhao G, Brune ME, Napier JJ, Mulhern MM, Lynch JK, Freeman JC, Wodka D, Chen CJ, Falls HD, Brodjian S, Dayton BD, Diaz GJ, Bush EN, Shapiro R, Droz BA, Knourek-Segel V, Hernandez LE, Marsh KC, Reilly RM, Sham HL, Collins CA, Kym PR.
Bioorg Med Chem Lett (2007) 17 : 884 -889
PubMed 17188866 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.71 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL214585 3 9.00
CHEMBL215661 3 8.52
CHEMBL214731 1 8.40
CHEMBL384111 1 7.96
CHEMBL384919 1 7.68
CHEMBL425257 1 7.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL214585 IC50 = 1.0 nM 9.00
CHEMBL215661 IC50 = 3.0 nM 8.52
CHEMBL214731 IC50 = 4.0 nM 8.40
CHEMBL215661 IC50 = 4.0 nM 8.40
CHEMBL214585 IC50 = 5.0 nM 8.30
CHEMBL384111 IC50 = 11.0 nM 7.96
CHEMBL384919 IC50 = 21.0 nM 7.68
CHEMBL425257 IC50 = 76.0 nM 7.12
CHEMBL214585 IC50 = 760.0 nM 6.12
CHEMBL215661 IC50 = 2570.0 nM 5.59