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Assay Detail

CHEMBL4019575

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

Functional
Antiproliferative activity against human HCT116/VP35 cells after 72 hrs by phosphatase assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HCT116/VP35
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Vinblastine 20' Amides: Synthetic Analogues That Maintain or Improve Potency and Simultaneously Overcome Pgp-Derived Efflux and Resistance.
Lukesh JC, Carney DW, Dong H, Cross RM, Shukla V, Duncan KK, Yang S, Brody DM, Brütsch MM, Radakovic A, Boger DL.
J Med Chem (2017) 60 : 7591 -7604
PubMed 28857558 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.19 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4069142 1 8.85
CHEMBL4088308 1 8.24
CHEMBL4091990 1 8.21
CHEMBL428647 PACLITAXEL 4.0 1 8.20
CHEMBL159 VINBLASTINE 4.0 1 7.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4069142 IC50 = 1.4 nM 8.85
CHEMBL4088308 IC50 = 5.8 nM 8.24
CHEMBL4091990 IC50 = 6.2 nM 8.21
CHEMBL428647 PACLITAXEL IC50 = 6.3 nM 8.20
CHEMBL159 VINBLASTINE IC50 = 37.0 nM 7.43