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Assay Detail

CHEMBL4812677

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

ADMET
Inhibition of CYP3A4 (unknown origin) by UPLC-MS analysis
5
Total Activities
5
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

Potent Antimalarials with Development Potential Identified by Structure-Guided Computational Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series.
Palmer MJ, Deng X, Watts S, Krilov G, Gerasyuto A, Kokkonda S, El Mazouni F, White J, White KL, Striepen J, Bath J, Schindler KA, Yeo T, Shackleford DM, Mok S, Deni I, Lawong A, Huang A, Chen G, Wang W, Jayaseelan J, Katneni K, Patil R, Saunders J, Shahi SP, Chittimalla R, Angulo-Barturen I, Jiménez-Díaz MB, Wittlin S, Tumwebaze PK, Rosenthal PJ, Cooper RA, Aguiar ACC, Guido RVC, Pereira DB, Mittal N, Winzeler EA, Tomchick DR, Laleu B, Burrows JN, Rathod PK, Fidock DA, Charman SA, Phillips MA.
J Med Chem (2021) 64 : 6085 -6136
PubMed 33876936 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.42 5.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4851471 1 5.77
CHEMBL4850393 1 5.07
CHEMBL4850116 1 -
CHEMBL4848632 1 -
CHEMBL4876457 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4851471 IC50 = 1700.0 nM 5.77
CHEMBL4850393 IC50 = 8500.0 nM 5.07
CHEMBL4850116 IC50 > 20000.0 nM -
CHEMBL4848632 IC50 > 20000.0 nM -
CHEMBL4876457 IC50 > 20000.0 nM -