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Assay Detail

CHEMBL5365795

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Functional
Antiproliferative activity against human A2780 cells assessed as cell growth inhibition
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type A2780
Confidence 1 — Organism
Curated By Autocuration

Target

A2780 (CHEMBL614004)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of potent NAMPT-Targeting PROTACs using FK866 as the warhead.
Zhang P, Wang W, Guo M, Zhou L, Dong G, Xu D, Sheng C.
Bioorg Med Chem Lett (2023) 92 : 129393 -129393
PubMed 37369332 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.79 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5394343 1 8.62
CHEMBL5404254 1 8.52
CHEMBL5398077 1 8.23
CHEMBL5432491 1 7.51
CHEMBL5408614 1 7.47
CHEMBL5428751 1 7.42
CHEMBL5401142 1 7.39
CHEMBL5408297 1 7.16
CHEMBL566757 DAPORINAD 2.0 1 -
CHEMBL5434442 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5394343 IC50 = 2.4 nM 8.62
CHEMBL5404254 IC50 = 3.0 nM 8.52
CHEMBL5398077 IC50 = 5.9 nM 8.23
CHEMBL5432491 IC50 = 30.6 nM 7.51
CHEMBL5408614 IC50 = 33.7 nM 7.47
CHEMBL5428751 IC50 = 37.9 nM 7.42
CHEMBL5401142 IC50 = 41.1 nM 7.39
CHEMBL5408297 IC50 = 69.2 nM 7.16
CHEMBL566757 DAPORINAD IC50 < 3.0 nM -
CHEMBL5434442 IC50 < 4.0 nM -