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Assay Detail

CHEMBL4830385

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Functional
Antiproliferative activity against human A375/TxR cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type A375/TxR
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

X-ray Crystallography-Guided Design, Antitumor Efficacy, and QSAR Analysis of Metabolically Stable Cyclopenta-Pyrimidinyl Dihydroquinoxalinone as a Potent Tubulin Polymerization Inhibitor.
Banerjee S, Mahmud F, Deng S, Ma L, Yun MK, Fakayode SO, Arnst KE, Yang L, Chen H, Wu Z, Lukka PB, Parmar K, Meibohm B, White SW, Wang Y, Li W, Miller DD.
J Med Chem (2021) 64 : 13072 -13095
PubMed 34406768 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.32 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL492399 VERUBULIN 2.0 1 9.15
CHEMBL4855608 1 8.96
CHEMBL4871913 1 8.89
CHEMBL107 COLCHICINE 4.0 1 7.63
CHEMBL428647 PACLITAXEL 4.0 1 6.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL492399 VERUBULIN IC50 = 0.7 nM 9.15
CHEMBL4855608 IC50 = 1.1 nM 8.96
CHEMBL4871913 IC50 = 1.3 nM 8.89
CHEMBL107 COLCHICINE IC50 = 23.6 nM 7.63
CHEMBL428647 PACLITAXEL IC50 = 103.8 nM 6.98