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Assay Detail

CHEMBL3585200

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

ADMET
Inhibition of CYP3A4 (unknown origin)
17
Total Activities
17
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

Design, Synthesis, and Structure-Activity Relationships of Pyridine-Based Rho Kinase (ROCK) Inhibitors.
Green J, Cao J, Bandarage UK, Gao H, Court J, Marhefka C, Jacobs M, Taslimi P, Newsome D, Nakayama T, Shah S, Rodems S.
J Med Chem (2015) 58 : 5028 -5037
PubMed 26039570 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 5.38 6.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3581132 1 6.32
CHEMBL3581121 1 6.12
CHEMBL3581144 1 5.82
CHEMBL3581138 1 5.70
CHEMBL3581142 1 5.46
CHEMBL3581145 1 5.44
CHEMBL3581146 1 5.42
CHEMBL3581147 1 5.30
CHEMBL3581149 1 5.25
CHEMBL3581139 1 5.13
CHEMBL3581148 1 5.12
CHEMBL3581143 1 5.08
CHEMBL3581137 1 5.00
CHEMBL3581141 1 4.94
CHEMBL3581140 1 4.58
CHEMBL3580669 1 -
CHEMBL3581150 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3581132 IC50 = 480.0 nM 6.32
CHEMBL3581121 IC50 = 750.0 nM 6.12
CHEMBL3581144 IC50 = 1500.0 nM 5.82
CHEMBL3581138 IC50 = 2000.0 nM 5.70
CHEMBL3581142 IC50 = 3500.0 nM 5.46
CHEMBL3581145 IC50 = 3600.0 nM 5.44
CHEMBL3581146 IC50 = 3800.0 nM 5.42
CHEMBL3581147 IC50 = 5000.0 nM 5.30
CHEMBL3581149 IC50 = 5600.0 nM 5.25
CHEMBL3581139 IC50 = 7400.0 nM 5.13
CHEMBL3581148 IC50 = 7500.0 nM 5.12
CHEMBL3581143 IC50 = 8300.0 nM 5.08
CHEMBL3581137 IC50 = 10000.0 nM 5.00
CHEMBL3581141 IC50 = 11400.0 nM 4.94
CHEMBL3581140 IC50 = 26000.0 nM 4.58
CHEMBL3580669 IC50 > 30000.0 nM -
CHEMBL3581150 IC50 > 15000.0 nM -