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Assay Detail

CHEMBL5320108

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

Binding
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in CHO cells measured for 2 hrs by microbeta counter analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Melanocortin receptor 3 (CHEMBL4644)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of the Potent and Selective MC4R Antagonist PF-07258669 for the Potential Treatment of Appetite Loss.
Garnsey MR, Smith AC, Polivkova J, Arons AL, Bai G, Blakemore C, Boehm M, Buzon LM, Campion SN, Cerny M, Chang SC, Coffman K, Farley KA, Fonseca KR, Ford KK, Garren J, Kong JX, Koos MRM, Kung DW, Lian Y, Li MM, Li Q, Martinez-Alsina LA, O'Connor R, Ogilvie K, Omoto K, Raymer B, Reese MR, Ryder T, Samp L, Stevens KA, Widlicka DW, Yang Q, Zhu K, Fortin JP, Sammons MF.
J Med Chem (2023) 66 : 3195 -3211
PubMed 36802610 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 6.47 6.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5432266 1 6.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5432266 Ki = 340.0 nM 6.47