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Assay Detail

CHEMBL4359684

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

Functional
Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by SRB assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HCT-116
Confidence 1 — Organism
Curated By Autocuration

Target

HCT-116 (CHEMBL394)
Type CELL-LINE
Organism Homo sapiens

Publication

Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation.
Zhu S, Shen Q, Gao Y, Wang L, Fang Y, Chen Y, Lu W.
J Med Chem (2020) 63 : 5421 -5441
PubMed 32352777 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.10 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL837 7-ETHYL-10-HYDROXYCAMPTOTHECIN 2.0 1 8.40
CHEMBL4460245 1 7.66
CHEMBL4436271 1 7.08
CHEMBL252164 LUMINESPIB 2.0 1 6.92
CHEMBL481 IRINOTECAN 4.0 1 6.30
CHEMBL4446403 1 6.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL837 7-ETHYL-10-HYDROXYCAMPTOTHECIN IC50 = 4.0 nM 8.40
CHEMBL4460245 IC50 = 22.0 nM 7.66
CHEMBL4436271 IC50 = 83.0 nM 7.08
CHEMBL252164 LUMINESPIB IC50 = 121.0 nM 6.92
CHEMBL481 IRINOTECAN IC50 = 498.0 nM 6.30
CHEMBL4446403 IC50 = 614.0 nM 6.21