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Assay Detail

CHEMBL871632

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

Binding
Displacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assay
16
Total Activities
16
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 2 (CHEMBL5038)
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 16 8.21 8.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL196667 1 8.43
CHEMBL194408 1 8.35
CHEMBL197026 1 8.33
CHEMBL195635 1 8.20
CHEMBL197050 1 8.19
CHEMBL427540 1 8.17
CHEMBL373084 1 8.17
CHEMBL196581 1 8.15
CHEMBL196196 1 8.08
CHEMBL194837 1 8.06
CHEMBL198361 1 -
CHEMBL195351 1 -
CHEMBL194691 1 -
CHEMBL197245 1 -
CHEMBL196567 1 -
CHEMBL187756 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL196667 IC50 = 3.7 nM 8.43
CHEMBL194408 IC50 = 4.5 nM 8.35
CHEMBL197026 IC50 = 4.7 nM 8.33
CHEMBL195635 IC50 = 6.3 nM 8.20
CHEMBL197050 IC50 = 6.4 nM 8.19
CHEMBL427540 IC50 = 6.8 nM 8.17
CHEMBL373084 IC50 = 6.8 nM 8.17
CHEMBL196581 IC50 = 7.1 nM 8.15
CHEMBL196196 IC50 = 8.4 nM 8.08
CHEMBL194837 IC50 = 8.7 nM 8.06
CHEMBL198361 IC50 > 10.0 nM -
CHEMBL195351 IC50 > 10.0 nM -
CHEMBL194691 IC50 > 10.0 nM -
CHEMBL197245 IC50 > 10.0 nM -
CHEMBL196567 IC50 > 10.0 nM -
CHEMBL187756 IC50 > 10.0 nM -