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Assay Detail

CHEMBL898579

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

ADMET
Inhibition of CYP3A4
28
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Rational design of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as small molecule renin inhibitors.
Powell NA, Ciske FL, Cai C, Holsworth DD, Mennen K, Van Huis CA, Jalaie M, Day J, Mastronardi M, McConnell P, Mochalkin I, Zhang E, Ryan MJ, Bryant J, Collard W, Ferreira S, Gu C, Collins R, Edmunds JJ.
Bioorg Med Chem (2007) 15 : 5912 -5949
PubMed 17574423 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 5.98 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL393363 1 6.92
CHEMBL240598 1 6.80
CHEMBL241241 1 6.57
CHEMBL239497 1 6.34
CHEMBL239085 1 6.28
CHEMBL239074 1 6.23
CHEMBL241032 1 6.17
CHEMBL398584 2 6.07
CHEMBL238866 1 6.04
CHEMBL393109 1 5.97
CHEMBL239496 2 5.94
CHEMBL240391 1 5.78
CHEMBL241663 1 5.77
CHEMBL239078 1 5.72
CHEMBL240813 1 5.66
CHEMBL239495 1 5.52
CHEMBL429459 1 5.32
CHEMBL393218 1 4.52
CHEMBL391463 1 -
CHEMBL398811 1 -
CHEMBL429642 1 -
CHEMBL400431 1 -
CHEMBL398387 1 -
CHEMBL240566 1 -
CHEMBL394016 1 -
CHEMBL240355 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL393363 IC50 = 120.0 nM 6.92
CHEMBL240598 IC50 = 160.0 nM 6.80
CHEMBL241241 IC50 = 270.0 nM 6.57
CHEMBL239497 IC50 = 460.0 nM 6.34
CHEMBL239085 IC50 = 530.0 nM 6.28
CHEMBL239074 IC50 = 590.0 nM 6.23
CHEMBL241032 IC50 = 670.0 nM 6.17
CHEMBL398584 IC50 = 860.0 nM 6.07
CHEMBL398584 IC50 = 860.0 nM 6.07
CHEMBL238866 IC50 = 920.0 nM 6.04
CHEMBL393109 IC50 = 1060.0 nM 5.97
CHEMBL239496 IC50 = 1140.0 nM 5.94
CHEMBL239496 IC50 = 1140.0 nM 5.94
CHEMBL240391 IC50 = 1670.0 nM 5.78
CHEMBL241663 IC50 = 1700.0 nM 5.77
CHEMBL239078 IC50 = 1900.0 nM 5.72
CHEMBL240813 IC50 = 2180.0 nM 5.66
CHEMBL239495 IC50 = 3000.0 nM 5.52
CHEMBL429459 IC50 = 4790.0 nM 5.32
CHEMBL393218 IC50 = 30000.0 nM 4.52
CHEMBL391463 IC50 > 30000.0 nM -
CHEMBL398811 IC50 > 30000.0 nM -
CHEMBL429642 IC50 > 30000.0 nM -
CHEMBL400431 IC50 > 30000.0 nM -
CHEMBL398387 IC50 > 30000.0 nM -
CHEMBL240566 IC50 > 30000.0 nM -
CHEMBL394016 IC50 > 22000.0 nM -
CHEMBL240355 IC50 > 30000.0 nM -