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Assay Detail

CHEMBL4317009

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

ADMET
Reversible inhibition of CYP3A4 (unknown origin) using midazolam as substrate
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cytochrome P450 3A4 (CHEMBL340)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma.
Wang X, Blackaby W, Allen V, Chan GKY, Chang JH, Chiang PC, Diène C, Drummond J, Do S, Fan E, Harstad EB, Hodges A, Hu H, Jia W, Kofie W, Kolesnikov A, Lyssikatos JP, Ly J, Matteucci M, Moffat JG, Munugalavadla V, Murray J, Nash D, Noland CL, Del Rosario G, Ross L, Rouse C, Sharpe A, Slaga D, Sun M, Tsui V, Wallweber H, Yu SF, Ebens AJ.
J Med Chem (2019) 62 : 2140 -2153
PubMed 30715878 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.27 5.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3623150 1 5.42
CHEMBL3648680 1 5.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3623150 IC50 = 3800.0 nM 5.42
CHEMBL3648680 IC50 = 7500.0 nM 5.12