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Assay Detail

CHEMBL993705

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Functional
Antagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assay
5
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Novel approach for chemotype hopping based on annotated databases of chemically feasible fragments and a prospective case study: new melanin concentrating hormone antagonists.
Oyarzabal J, Howe T, Alcazar J, Andrés JI, Alvarez RM, Dautzenberg F, Iturrino L, Martínez S, Van der Linden I.
J Med Chem (2009) 52 : 2076 -2089
PubMed 19290642 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.11 7.34
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL470633 1 7.34
CHEMBL512873 1 7.08
CHEMBL214957 2 7.05
CHEMBL470840 1 6.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL470633 IC50 = 45.71 nM 7.34
CHEMBL512873 IC50 = 83.18 nM 7.08
CHEMBL214957 IC50 = 89.13 nM 7.05
CHEMBL470840 IC50 = 104.71 nM 6.98
CHEMBL214957 Activity = 87.0 nM -