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Assay Detail

CHEMBL860697

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

Binding
Displacement of [125I]MCH from MCHr1 expressed in IMR32 (I3.4.2) cells
16
Total Activities
16
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

Screening for cardiovascular safety: a structure-activity approach for guiding lead selection of melanin concentrating hormone receptor 1 antagonists.
Kym PR, Souers AJ, Campbell TJ, Lynch JK, Judd AS, Iyengar R, Vasudevan A, Gao J, Freeman JC, Wodka D, Mulhern M, Zhao G, Wagaw SH, Napier JJ, Brodjian S, Dayton BD, Reilly RM, Segreti JA, Fryer RM, Preusser LC, Reinhart GA, Hernandez L, Marsh KC, Sham HL, Collins CA, Polakowski JS.
J Med Chem (2006) 49 : 2339 -2352
PubMed 16570930 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.77 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL179501 1 8.85
CHEMBL194697 1 8.70
CHEMBL196208 1 8.70
CHEMBL204828 1 8.52
CHEMBL380429 1 8.40
CHEMBL383078 1 8.30
CHEMBL206081 1 8.22
CHEMBL426666 1 8.00
CHEMBL426292 1 7.92
CHEMBL383359 1 7.80
CHEMBL360142 1 7.60
CHEMBL202741 1 7.34
CHEMBL383076 1 7.24
CHEMBL380144 1 7.11
CHEMBL180168 1 6.25
CHEMBL205106 1 5.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL179501 IC50 = 1.4 nM 8.85
CHEMBL194697 IC50 = 2.0 nM 8.70
CHEMBL196208 IC50 = 2.0 nM 8.70
CHEMBL204828 IC50 = 3.0 nM 8.52
CHEMBL380429 IC50 = 4.0 nM 8.40
CHEMBL383078 IC50 = 5.0 nM 8.30
CHEMBL206081 IC50 = 6.0 nM 8.22
CHEMBL426666 IC50 = 10.0 nM 8.00
CHEMBL426292 IC50 = 12.0 nM 7.92
CHEMBL383359 IC50 = 16.0 nM 7.80
CHEMBL360142 IC50 = 25.0 nM 7.60
CHEMBL202741 IC50 = 46.0 nM 7.34
CHEMBL383076 IC50 = 57.0 nM 7.24
CHEMBL380144 IC50 = 78.0 nM 7.11
CHEMBL180168 IC50 = 558.0 nM 6.25
CHEMBL205106 IC50 = 3628.0 nM 5.44