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Assay Detail

CHEMBL834393

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

Functional
Concentration required to inhibit growth of human cervical HeLa carcinoma cell line
17
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HeLa
Confidence 1 — Organism
Curated By Intermediate

Target

HeLa (CHEMBL399)
Type CELL-LINE
Organism Homo sapiens

Publication

Camptothecin analogs with bulky, hydrophobic substituents at the 7-position via a Grignard reaction.
Manikumar G, Wadkins RM, Bearss D, Von Hoff DD, Wani MC, Wall ME.
Bioorg Med Chem Lett (2004) 14 : 5377 -5381
PubMed 15454230 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.60 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL361594 1 8.70
CHEMBL181547 1 8.21
CHEMBL364360 1 8.16
CHEMBL184094 1 8.09
CHEMBL359567 1 8.05
CHEMBL307794 1 8.02
CHEMBL183350 1 7.86
CHEMBL360812 1 7.79
CHEMBL363752 1 7.69
CHEMBL837 7-ETHYL-10-HYDROXYCAMPTOTHECIN 2.0 2 7.59
CHEMBL185306 1 7.58
CHEMBL184100 1 7.43
CHEMBL188121 1 7.09
CHEMBL65 CAMPTOTHECIN -1.0 1 6.93
CHEMBL364827 1 6.69
CHEMBL186541 1 5.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL361594 IC50 = 2.0 nM 8.70
CHEMBL181547 IC50 = 6.2 nM 8.21
CHEMBL364360 IC50 = 6.9 nM 8.16
CHEMBL184094 IC50 = 8.1 nM 8.09
CHEMBL359567 IC50 = 9.0 nM 8.05
CHEMBL307794 IC50 = 9.6 nM 8.02
CHEMBL183350 IC50 = 13.9 nM 7.86
CHEMBL360812 IC50 = 16.2 nM 7.79
CHEMBL363752 IC50 = 20.5 nM 7.69
CHEMBL837 7-ETHYL-10-HYDROXYCAMPTOTHECIN IC50 = 25.7 nM 7.59
CHEMBL185306 IC50 = 26.0 nM 7.58
CHEMBL184100 IC50 = 37.3 nM 7.43
CHEMBL837 7-ETHYL-10-HYDROXYCAMPTOTHECIN IC50 = 38.8 nM 7.41
CHEMBL188121 IC50 = 80.9 nM 7.09
CHEMBL65 CAMPTOTHECIN IC50 = 117.2 nM 6.93
CHEMBL364827 IC50 = 204.1 nM 6.69
CHEMBL186541 IC50 = 1310.0 nM 5.88