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Assay Detail

CHEMBL3583384

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

Binding
Inhibition of human ERG by Patchexpress patch clamp assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes.
Shah SK, He S, Guo L, Truong Q, Qi H, Du W, Lai Z, Liu J, Jian T, Hong Q, Dobbelaar P, Ye Z, Sherer E, Feng Z, Yu Y, Wong F, Samuel K, Madiera M, Karanam BV, Reddy VB, Mitelman S, Tong SX, Chicchi GG, Tsao KL, Trusca D, Feng Y, Wu M, Shao Q, Trujillo ME, Eiermann GJ, Li C, Pachanski M, Fernandez G, Nelson D, Bunting P, Morissette P, Volksdorf S, Kerr J, Zhang BB, Howard AD, Zhou YP, Pasternak A, Nargund RP, Hagmann WK.
ACS Med Chem Lett (2015) 6 : 513 -517
PubMed 26005524 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 4.99 5.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2204935 1 5.47
CHEMBL3582317 1 4.92
CHEMBL3582336 1 4.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2204935 IC50 = 3400.0 nM 5.47
CHEMBL3582317 IC50 = 12000.0 nM 4.92
CHEMBL3582336 IC50 = 27000.0 nM 4.57