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Assay Detail

CHEMBL832325

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

Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 3.
Souers AJ, Wodka D, Gao J, Lewis JC, Vasudevan A, Brodjian S, Dayton B, Ogiela CA, Fry D, Hernandez LE, Marsh KC, Collins CA, Kym PR.
Bioorg Med Chem Lett (2004) 14 : 4883 -4886
PubMed 15341944 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 7.62 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL181813 1 9.05
CHEMBL362009 1 9.00
CHEMBL186548 1 8.92
CHEMBL363909 1 8.66
CHEMBL362501 1 8.57
CHEMBL182261 1 8.52
CHEMBL363664 1 8.30
CHEMBL184609 1 7.69
CHEMBL364983 1 7.59
CHEMBL364540 1 7.41
CHEMBL185266 1 7.39
CHEMBL185558 1 7.16
CHEMBL360620 1 7.16
CHEMBL364377 1 7.05
CHEMBL183468 1 7.05
CHEMBL361305 1 6.92
CHEMBL184277 1 6.83
CHEMBL184482 1 6.68
CHEMBL365876 1 6.24
CHEMBL184437 1 6.14
CHEMBL184692 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL181813 IC50 = 0.9 nM 9.05
CHEMBL362009 IC50 = 1.0 nM 9.00
CHEMBL186548 IC50 = 1.2 nM 8.92
CHEMBL363909 IC50 = 2.2 nM 8.66
CHEMBL362501 IC50 = 2.7 nM 8.57
CHEMBL182261 IC50 = 3.0 nM 8.52
CHEMBL363664 IC50 = 5.0 nM 8.30
CHEMBL184609 IC50 = 20.5 nM 7.69
CHEMBL364983 IC50 = 25.6 nM 7.59
CHEMBL364540 IC50 = 38.6 nM 7.41
CHEMBL185266 IC50 = 41.0 nM 7.39
CHEMBL185558 IC50 = 70.0 nM 7.16
CHEMBL360620 IC50 = 70.0 nM 7.16
CHEMBL364377 IC50 = 90.0 nM 7.05
CHEMBL183468 IC50 = 90.0 nM 7.05
CHEMBL361305 IC50 = 120.0 nM 6.92
CHEMBL184277 IC50 = 149.0 nM 6.83
CHEMBL184482 IC50 = 210.0 nM 6.68
CHEMBL365876 IC50 = 580.0 nM 6.24
CHEMBL184437 IC50 = 730.0 nM 6.14
CHEMBL184692 IC50 > 2000.0 nM -