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Assay Detail

CHEMBL5336082

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

Functional
Antitumor activity in human MIA PaCa-2 cells assessed as intracellular NAD+ depletion incubated for 24 hrs by enzymatic cycling assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MIA PaCa-2
Confidence 1 — Organism
Curated By Autocuration

Target

MIA PaCa-2 (CHEMBL614725)
Type CELL-LINE
Organism Homo sapiens

Publication

Synthesis and structure-activity relationship of new nicotinamide phosphoribosyltransferase inhibitors with antitumor activity on solid and haematological cancer.
Fratta S, Biniecka P, Moreno-Vargas AJ, Carmona AT, Nahimana A, Duchosal MA, Piacente F, Bruzzone S, Caffa I, Nencioni A, Robina I.
Eur J Med Chem (2023) 250 : 115170 -115170
PubMed 36787658 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 9.08 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5413890 1 9.85
CHEMBL5431155 1 9.77
CHEMBL5433246 1 9.70
CHEMBL5428441 1 9.60
CHEMBL566757 DAPORINAD 2.0 1 9.47
CHEMBL5396894 1 9.37
CHEMBL5409679 1 9.30
CHEMBL5421145 1 9.06
CHEMBL5417778 1 8.85
CHEMBL5416318 1 8.83
CHEMBL5439639 1 8.82
CHEMBL5418853 1 8.70
CHEMBL5422822 1 8.63
CHEMBL5406214 1 8.33
CHEMBL5441013 1 7.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5413890 IC50 = 0.14 nM 9.85
CHEMBL5431155 IC50 = 0.17 nM 9.77
CHEMBL5433246 IC50 = 0.2 nM 9.70
CHEMBL5428441 IC50 = 0.25 nM 9.60
CHEMBL566757 DAPORINAD IC50 = 0.34 nM 9.47
CHEMBL5396894 IC50 = 0.43 nM 9.37
CHEMBL5409679 IC50 = 0.5 nM 9.30
CHEMBL5421145 IC50 = 0.88 nM 9.06
CHEMBL5417778 IC50 = 1.43 nM 8.85
CHEMBL5416318 IC50 = 1.48 nM 8.83
CHEMBL5439639 IC50 = 1.5 nM 8.82
CHEMBL5418853 IC50 = 2.0 nM 8.70
CHEMBL5422822 IC50 = 2.36 nM 8.63
CHEMBL5406214 IC50 = 4.7 nM 8.33
CHEMBL5441013 IC50 = 11.25 nM 7.95