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Assay Detail

CHEMBL2377957

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

Functional
Antiproliferative activity against HDFa cells after 30 hrs by [3H]-thymidine incorporation assay
8
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Pyridinylquinazolines selectively inhibit human methionine aminopeptidase-1 in cells.
Zhang F, Bhat S, Gabelli SB, Chen X, Miller MS, Nacev BA, Cheng YL, Meyers DJ, Tenney K, Shim JS, Crews P, Amzel LM, Ma D, Liu JO.
J Med Chem (2013) 56 : 3996 -4016
PubMed 23634668 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 5.76 6.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL327579 2 6.19
CHEMBL2375627 1 6.12
CHEMBL2375628 1 5.72
CHEMBL2375624 1 5.72
CHEMBL472879 1 5.44
CHEMBL39879 DIPYRIDYL 1 5.00
CHEMBL625 THIABENDAZOLE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL327579 EC50 = 650.0 nM 6.19
CHEMBL2375627 EC50 = 760.0 nM 6.12
CHEMBL327579 EC50 = 790.0 nM 6.10
CHEMBL2375628 EC50 = 1900.0 nM 5.72
CHEMBL2375624 EC50 = 1900.0 nM 5.72
CHEMBL472879 EC50 = 3600.0 nM 5.44
CHEMBL39879 DIPYRIDYL EC50 = 10000.0 nM 5.00
CHEMBL625 THIABENDAZOLE EC50 > 250000.0 nM -