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Assay Detail

CHEMBL2167058

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

Functional
Cytotoxicity against human KB cells after 2 hrs by methylene blue staining-based spectrophotometric analysis
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

KB (CHEMBL398)
Type CELL-LINE
Organism Homo sapiens

Publication

Antitumor agents 295. E-ring hydroxylated antofine and cryptopleurine analogues as antiproliferative agents: design, synthesis, and mechanistic studies.
Yang X, Shi Q, Lai CY, Chen CY, Ohkoshi E, Yang SC, Wang CY, Bastow KF, Wu TS, Pan SL, Teng CM, Yang PC, Lee KH.
J Med Chem (2012) 55 : 6751 -6761
PubMed 22823514 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.49 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL198075 CRYPTOPLEURINE 1 8.82
CHEMBL2164800 1 7.64
CHEMBL2164804 1 7.60
CHEMBL2164802 1 7.48
CHEMBL228286 (-)-ANTOFINE 1 7.44
CHEMBL2164799 1 7.37
CHEMBL2164798 1 7.30
CHEMBL2164791 1 7.00
CHEMBL2164805 1 6.52
CHEMBL2164795 1 6.30
CHEMBL2164793 1 6.30
CHEMBL2164801 1 6.13
CHEMBL2164796 1 6.11
CHEMBL2164806 1 6.08
CHEMBL2164808 1 6.04
CHEMBL2164797 1 5.74
CHEMBL2164792 1 5.74
CHEMBL2164803 1 5.65
CHEMBL2164809 1 5.28
CHEMBL2164794 1 4.92
CHEMBL2164807 1 4.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL198075 CRYPTOPLEURINE IC50 = 1.51 nM 8.82
CHEMBL2164800 IC50 = 23.0 nM 7.64
CHEMBL2164804 IC50 = 25.0 nM 7.60
CHEMBL2164802 IC50 = 33.0 nM 7.48
CHEMBL228286 (-)-ANTOFINE IC50 = 36.0 nM 7.44
CHEMBL2164799 IC50 = 43.0 nM 7.37
CHEMBL2164798 IC50 = 50.0 nM 7.30
CHEMBL2164791 IC50 = 100.0 nM 7.00
CHEMBL2164805 IC50 = 300.0 nM 6.52
CHEMBL2164795 IC50 = 500.0 nM 6.30
CHEMBL2164793 IC50 = 500.0 nM 6.30
CHEMBL2164801 IC50 = 734.0 nM 6.13
CHEMBL2164796 IC50 = 780.0 nM 6.11
CHEMBL2164806 IC50 = 840.0 nM 6.08
CHEMBL2164808 IC50 = 920.0 nM 6.04
CHEMBL2164797 IC50 = 1810.0 nM 5.74
CHEMBL2164792 IC50 = 1830.0 nM 5.74
CHEMBL2164803 IC50 = 2250.0 nM 5.65
CHEMBL2164809 IC50 = 5240.0 nM 5.28
CHEMBL2164794 IC50 = 12000.0 nM 4.92
CHEMBL2164807 IC50 = 17520.0 nM 4.76