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Assay Detail

CHEMBL4845068

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Binding
Inhibition of human MGAT2 in mouse STC-1 cell based assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type STC-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Screening Hit to Clinical Candidate: Discovery of BMS-963272, a Potent, Selective MGAT2 Inhibitor for the Treatment of Metabolic Disorders.
Turdi H, Chao H, Hangeland JJ, Ahmad S, Meng W, Brigance R, Zhao G, Wang W, Moore F, Ye XY, Mathur A, Hou X, Kempson J, Wu DR, Li YX, Azzara AV, Ma Z, Chu CH, Chen L, Cullen MJ, Rooney S, Harvey S, Kopcho L, Panemangelor R, Abell L, O'Malley K, Keim WJ, Dierks E, Chang S, Foster K, Apedo A, Harden D, Dabros M, Gao Q, Pelleymounter MA, Whaley JM, Robl JA, Cheng D, Lawrence RM, Devasthale P.
J Med Chem (2021) 64 : 14773 -14792
PubMed 34613725 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.19 9.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3893594 1 9.20
CHEMBL4878564 1 7.89
CHEMBL3912712 BMS-963272 1.0 1 7.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3893594 IC50 = 0.63 nM 9.20
CHEMBL4878564 IC50 = 13.0 nM 7.89
CHEMBL3912712 BMS-963272 IC50 = 33.0 nM 7.48