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Assay Detail

CHEMBL5320104

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Toxicity
Inhibition of hERG expressed in CHO cells stably at -80 mV holding potential by automated patch clamp method
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

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
IC50 6 4.83 6.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5416581 1 6.44
CHEMBL5437236 1 4.72
CHEMBL5411999 1 4.60
CHEMBL5432266 1 4.57
CHEMBL5411365 1 4.55
CHEMBL5403087 1 4.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5416581 IC50 = 360.0 nM 6.44
CHEMBL5437236 IC50 = 19000.0 nM 4.72
CHEMBL5411999 IC50 = 25000.0 nM 4.60
CHEMBL5432266 IC50 = 27000.0 nM 4.57
CHEMBL5411365 IC50 = 28000.0 nM 4.55
CHEMBL5403087 IC50 = 78000.0 nM 4.11