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Assay Detail

CHEMBL886902

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

Binding
Displacement of [125I]MCH from MCHR1 expressed in IMR32 cells
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type IMR-32
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Identification of diamino chromone-2-carboxamides as MCHr1 antagonists with minimal hERG channel activity.
Judd AS, Souers AJ, Wodka D, Zhao G, Mulhern MM, Iyengar RR, Gao J, Lynch JK, Freeman JC, Falls HD, Brodjian S, Dayton BD, Reilly RM, Gintant G, Limberis JT, Mikhail A, Leitza ST, Houseman KA, Diaz G, Bush EN, Shapiro R, Knourek-Segel V, Hernandez LE, Marsh KC, Sham HL, Collins CA, Kym PR.
Bioorg Med Chem Lett (2007) 17 : 2365 -2371
PubMed 17350253 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.62 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL246258 1 8.70
CHEMBL214021 1 8.52
CHEMBL248297 1 8.52
CHEMBL245844 1 8.40
CHEMBL394639 1 7.82
CHEMBL246050 1 7.77
CHEMBL248296 1 7.70
CHEMBL246464 1 7.64
CHEMBL214768 1 7.62
CHEMBL246259 1 7.58
CHEMBL245846 1 7.54
CHEMBL245642 1 7.51
CHEMBL247891 1 7.29
CHEMBL247689 1 7.19
CHEMBL246051 1 7.07
CHEMBL247688 1 6.78
CHEMBL248295 1 5.82
CHEMBL247690 1 -
CHEMBL247283 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL246258 IC50 = 2.0 nM 8.70
CHEMBL214021 IC50 = 3.0 nM 8.52
CHEMBL248297 IC50 = 3.0 nM 8.52
CHEMBL245844 IC50 = 4.0 nM 8.40
CHEMBL394639 IC50 = 15.0 nM 7.82
CHEMBL246050 IC50 = 17.0 nM 7.77
CHEMBL248296 IC50 = 20.0 nM 7.70
CHEMBL246464 IC50 = 23.0 nM 7.64
CHEMBL214768 IC50 = 24.0 nM 7.62
CHEMBL246259 IC50 = 26.0 nM 7.58
CHEMBL245846 IC50 = 29.0 nM 7.54
CHEMBL245642 IC50 = 31.0 nM 7.51
CHEMBL247891 IC50 = 51.0 nM 7.29
CHEMBL247689 IC50 = 64.0 nM 7.19
CHEMBL246051 IC50 = 86.0 nM 7.07
CHEMBL247688 IC50 = 165.0 nM 6.78
CHEMBL248295 IC50 = 1520.0 nM 5.82
CHEMBL247690 IC50 - -
CHEMBL247283 IC50 > 2000.0 nM -