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Assay Detail

CHEMBL3119735

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

ADMET
Inhibition of recombinant human CYP3A4
ChEMBL ↗
18
Total Activities
18
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

Discovery and optimization of pyrimidone indoline amide PI3Kβ inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers.
Certal V, Carry JC, Halley F, Virone-Oddos A, Thompson F, Filoche-Rommé B, El-Ahmad Y, Karlsson A, Charrier V, Delorme C, Rak A, Abecassis PY, Amara C, Vincent L, Bonnevaux H, Nicolas JP, Mathieu M, Bertrand T, Marquette JP, Michot N, Benard T, Perrin MA, Lemaitre O, Guerif S, Perron S, Monget S, Gruss-Leleu F, Doerflinger G, Guizani H, Brollo M, Delbarre L, Bertin L, Richepin P, Loyau V, Garcia-Echeverria C, Lengauer C, Schio L.
J Med Chem (2014) 57 : 903 -920
PubMed 24387221 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 4.44 4.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3112856 — — 1 4.96
CHEMBL3112858 — — 1 4.51
CHEMBL3112866 SAR-260301 1.0 1 4.40
CHEMBL3112865 — — 1 4.40
CHEMBL3112864 — — 1 4.40
CHEMBL3112861 — — 1 4.40
CHEMBL3112857 — — 1 4.40
CHEMBL3112855 — — 1 4.40
CHEMBL3112867 — — 1 4.40
CHEMBL3112853 — — 1 4.40
CHEMBL3112852 — — 1 4.40
CHEMBL3112850 — — 1 4.40
CHEMBL3112849 — — 1 4.40
CHEMBL3112848 — — 1 4.40
CHEMBL3112592 — — 1 4.40
CHEMBL3112847 — — 1 4.40
CHEMBL3112690 — — 1 4.40
CHEMBL3112854 — — 1 4.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3112856 — IC50 = 11000.0 nM 4.96
CHEMBL3112858 — IC50 = 31000.0 nM 4.51
CHEMBL3112866 SAR-260301 IC50 = 40000.0 nM 4.40
CHEMBL3112865 — IC50 = 40000.0 nM 4.40
CHEMBL3112864 — IC50 = 40000.0 nM 4.40
CHEMBL3112861 — IC50 = 40000.0 nM 4.40
CHEMBL3112857 — IC50 = 40000.0 nM 4.40
CHEMBL3112855 — IC50 = 40000.0 nM 4.40
CHEMBL3112867 — IC50 = 40000.0 nM 4.40
CHEMBL3112853 — IC50 = 40000.0 nM 4.40
CHEMBL3112852 — IC50 = 40000.0 nM 4.40
CHEMBL3112850 — IC50 = 40000.0 nM 4.40
CHEMBL3112849 — IC50 = 40000.0 nM 4.40
CHEMBL3112848 — IC50 = 40000.0 nM 4.40
CHEMBL3112592 — IC50 = 40000.0 nM 4.40
CHEMBL3112847 — IC50 = 40000.0 nM 4.40
CHEMBL3112690 — IC50 = 40000.0 nM 4.40
CHEMBL3112854 — IC50 = 40000.0 nM 4.40