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Assay Detail

CHEMBL1670542

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

ADMET
Inhibition of CYP3A4
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Spirodiketopiperazine-based CCR5 antagonist: discovery of an antiretroviral drug candidate.
Nishizawa R, Nishiyama T, Hisaichi K, Minamoto C, Matsunaga N, Takaoka Y, Nakai H, Jenkinson S, Kazmierski WM, Tada H, Sagawa K, Shibayama S, Fukushima D, Maeda K, Mitsuya H.
Bioorg Med Chem Lett (2011) 21 : 1141 -1145
PubMed 21256008 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 4.78 5.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL536743 1 5.03
CHEMBL537424 1 4.71
CHEMBL1170878 1 4.60
CHEMBL559168 1 -
CHEMBL536754 1 -
CHEMBL1668019 APLAVIROC HYDROCHLORIDE 3.0 1 -
CHEMBL1668020 1 -
CHEMBL1668021 1 -
CHEMBL1668022 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL536743 IC50 = 9300.0 nM 5.03
CHEMBL537424 IC50 = 19700.0 nM 4.71
CHEMBL1170878 IC50 = 24900.0 nM 4.60
CHEMBL559168 IC50 > 30000.0 nM -
CHEMBL536754 IC50 > 30000.0 nM -
CHEMBL1668019 APLAVIROC HYDROCHLORIDE IC50 > 30000.0 nM -
CHEMBL1668020 IC50 > 30000.0 nM -
CHEMBL1668021 IC50 > 30000.0 nM -
CHEMBL1668022 IC50 > 30000.0 nM -