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Assay Detail

CHEMBL856410

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

ADMET
P450 isoforms 3A4
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

ADMET (CHEMBL612558)
Type ADMET

Publication

Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase.
Mortlock AA, Foote KM, Heron NM, Jung FH, Pasquet G, Lohmann JJ, Warin N, Renaud F, De Savi C, Roberts NJ, Johnson T, Dousson CB, Hill GB, Perkins D, Hatter G, Wilkinson RW, Wedge SR, Heaton SP, Odedra R, Keen NJ, Crafter C, Brown E, Thompson K, Brightwell S, Khatri L, Brady MC, Kearney S, McKillop D, Rhead S, Parry T, Green S.
J Med Chem (2007) 50 : 2213 -2224
PubMed 17373783 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.26 5.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL214849 1 5.47
CHEMBL215022 1 5.19
CHEMBL385049 1 5.12
CHEMBL215152 DEFOSBARASERTIB 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL214849 IC50 = 3400.0 nM 5.47
CHEMBL215022 IC50 = 6400.0 nM 5.19
CHEMBL385049 IC50 = 7500.0 nM 5.12
CHEMBL215152 DEFOSBARASERTIB IC50 > 10000.0 nM -