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Assay Detail

CHEMBL871627

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

Binding
Displacement of 15 pM [125I]MCH from human MCH1R expressed in CHO-K1 in whole-cell binding assay
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

6-Acylamino-2-aminoquinolines as potent melanin-concentrating hormone 1 receptor antagonists. Identification, structure-activity relationship, and investigation of binding mode.
Ulven T, Frimurer TM, Receveur JM, Little PB, Rist O, Nørregaard PK, Högberg T.
J Med Chem (2005) 48 : 5684 -5697
PubMed 16134937 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 7.98 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL197050 1 9.05
CHEMBL370120 1 9.04
CHEMBL197026 1 8.82
CHEMBL195635 1 8.82
CHEMBL198361 1 8.80
CHEMBL427540 1 8.72
CHEMBL197245 1 8.68
CHEMBL184084 1 8.64
CHEMBL196567 1 8.64
CHEMBL194459 1 8.64
CHEMBL196581 1 8.57
CHEMBL196196 1 8.52
CHEMBL195351 1 8.40
CHEMBL194046 1 8.37
CHEMBL196667 1 8.30
CHEMBL196091 1 8.26
CHEMBL194408 1 8.23
CHEMBL373084 1 8.21
CHEMBL193473 1 8.21
CHEMBL187756 1 8.19
CHEMBL194691 1 8.06
CHEMBL189118 1 7.80
CHEMBL194477 1 7.70
CHEMBL197145 1 7.54
CHEMBL435494 1 7.54
CHEMBL196627 1 7.30
CHEMBL194837 1 7.07
CHEMBL195250 1 7.00
CHEMBL195022 1 6.96
CHEMBL382755 1 6.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL197050 IC50 = 0.9 nM 9.05
CHEMBL370120 IC50 = 0.92 nM 9.04
CHEMBL197026 IC50 = 1.5 nM 8.82
CHEMBL195635 IC50 = 1.5 nM 8.82
CHEMBL198361 IC50 = 1.6 nM 8.80
CHEMBL427540 IC50 = 1.9 nM 8.72
CHEMBL197245 IC50 = 2.1 nM 8.68
CHEMBL184084 IC50 = 2.3 nM 8.64
CHEMBL196567 IC50 = 2.3 nM 8.64
CHEMBL194459 IC50 = 2.3 nM 8.64
CHEMBL196581 IC50 = 2.7 nM 8.57
CHEMBL196196 IC50 = 3.0 nM 8.52
CHEMBL195351 IC50 = 4.0 nM 8.40
CHEMBL194046 IC50 = 4.3 nM 8.37
CHEMBL196667 IC50 = 5.0 nM 8.30
CHEMBL196091 IC50 = 5.5 nM 8.26
CHEMBL194408 IC50 = 5.9 nM 8.23
CHEMBL373084 IC50 = 6.1 nM 8.21
CHEMBL193473 IC50 = 6.1 nM 8.21
CHEMBL187756 IC50 = 6.4 nM 8.19
CHEMBL194691 IC50 = 8.7 nM 8.06
CHEMBL189118 IC50 = 16.0 nM 7.80
CHEMBL194477 IC50 = 20.0 nM 7.70
CHEMBL197145 IC50 = 29.0 nM 7.54
CHEMBL435494 IC50 = 29.0 nM 7.54
CHEMBL196627 IC50 = 50.0 nM 7.30
CHEMBL194837 IC50 = 85.0 nM 7.07
CHEMBL195250 IC50 = 100.0 nM 7.00
CHEMBL195022 IC50 = 111.0 nM 6.96
CHEMBL382755 IC50 = 151.0 nM 6.82
CHEMBL370820 IC50 = 158.0 nM 6.80
CHEMBL196360 IC50 = 302.0 nM 6.52
CHEMBL194484 IC50 = 5360.0 nM 5.27