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Assay Detail

CHEMBL1069510

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

Functional
Cytotoxicity against human KBM5 cells harboring wild type Bcr-Abl after 72 hrs by MTS assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type KBM5
Confidence 1 — Organism
Curated By Autocuration

Publication

Design, synthesis, and biological evaluation of novel water-soluble triptolide derivatives: Antineoplastic activity against imatinib-resistant CML cells bearing T315I mutant Bcr-Abl.
Xu F, Shi X, Li S, Cui J, Lu Z, Jin Y, Lin Y, Pang J, Pan J.
Bioorg Med Chem (2010) 18 : 1806 -1815
PubMed 20149665 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.85 7.99

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL463763 TRIPTOLIDE 3.0 1 7.99
CHEMBL604909 1 7.74
CHEMBL599250 1 7.73
CHEMBL596792 1 7.72
CHEMBL603470 1 7.57
CHEMBL597807 1 7.49
CHEMBL597806 1 7.33
CHEMBL599862 1 7.29
CHEMBL597404 1 7.28
CHEMBL598018 1 7.11
CHEMBL589202 1 6.53
CHEMBL597604 1 6.49
CHEMBL603883 1 6.46
CHEMBL598641 1 6.30
CHEMBL598640 1 6.11
CHEMBL603683 1 5.55
CHEMBL592716 1 5.30
CHEMBL589248 1 5.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL463763 TRIPTOLIDE IC50 = 10.3 nM 7.99
CHEMBL604909 IC50 = 18.2 nM 7.74
CHEMBL599250 IC50 = 18.6 nM 7.73
CHEMBL596792 IC50 = 19.2 nM 7.72
CHEMBL603470 IC50 = 27.2 nM 7.57
CHEMBL597807 IC50 = 32.2 nM 7.49
CHEMBL597806 IC50 = 46.7 nM 7.33
CHEMBL599862 IC50 = 51.3 nM 7.29
CHEMBL597404 IC50 = 52.5 nM 7.28
CHEMBL598018 IC50 = 78.0 nM 7.11
CHEMBL589202 IC50 = 297.0 nM 6.53
CHEMBL597604 IC50 = 327.1 nM 6.49
CHEMBL603883 IC50 = 348.0 nM 6.46
CHEMBL598641 IC50 = 496.0 nM 6.30
CHEMBL598640 IC50 = 774.0 nM 6.11
CHEMBL603683 IC50 = 2800.0 nM 5.55
CHEMBL592716 IC50 = 5020.0 nM 5.30
CHEMBL589248 IC50 = 5420.0 nM 5.27