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Assay Detail

CHEMBL3389571

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ADMET
Cytotoxicity against PHA-stimulated human PBMC by 5-bromo-2'-deoxyuridine incorporation assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Cell Type PBMC
Confidence 1 — Organism
Curated By Autocuration

Target

PBMC (CHEMBL613107)
Type CELL-LINE
Organism Homo sapiens

Publication

Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition.
Fu J, Tjandra M, Becker C, Bednarczyk D, Capparelli M, Elling R, Hanna I, Fujimoto R, Furegati M, Karur S, Kasprzyk T, Knapp M, Leung K, Li X, Lu P, Mergo W, Miault C, Ng S, Parker D, Peng Y, Roggo S, Rivkin A, Simmons RL, Wang M, Wiedmann B, Weiss AH, Xiao L, Xie L, Xu W, Yifru A, Yang S, Zhou B, Sweeney ZK.
J Med Chem (2014) 57 : 8503 -8516
PubMed 25310383 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.53 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1651956 ALISPORIVIR 3.0 1 6.30
CHEMBL1688529 NIM811 2.0 1 5.62
CHEMBL1269597 SCY 635 2.0 1 5.33
CHEMBL3344501 1 4.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1651956 ALISPORIVIR IC50 = 500.0 nM 6.30
CHEMBL1688529 NIM811 IC50 = 2400.0 nM 5.62
CHEMBL1269597 SCY 635 IC50 = 4700.0 nM 5.33
CHEMBL3344501 IC50 = 13200.0 nM 4.88