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Assay Detail

CHEMBL1805766

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Binding
Inhibition of nicotinamide phosphoribosyltransferase-catalyzed conversion of nicotinamide to nicotinamide mononucleotide
ChEMBL ↗
53
Total Activities
53
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Nicotinamide phosphoribosyltransferase (CHEMBL1744525) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Analogues of 4-[(7-Bromo-2-methyl-4-oxo-3H-quinazolin-6-yl)methylprop-2-ynylamino]-N-(3-pyridylmethyl)benzamide (CB-30865) as potent inhibitors of nicotinamide phosphoribosyltransferase (Nampt).
Lockman JW, Murphy BR, Zigar DF, Judd WR, Slattum PM, Gao ZH, Ostanin K, Green J, McKinnon R, Terry-Lorenzo RT, Fleischer TC, Boniface JJ, Shenderovich M, Willardsen JA.
J Med Chem (2010) 53 : 8734 -8746
PubMed 21080724 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 53 7.60 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1801863 — — 1 9.52
CHEMBL123756 — — 1 9.51
CHEMBL1801864 — — 1 9.35
CHEMBL1801934 — — 1 9.26
CHEMBL1801862 — — 1 9.10
CHEMBL1801566 — — 1 8.92
CHEMBL1801561 — — 1 8.89
CHEMBL1801552 — — 1 8.85
CHEMBL1801563 — — 1 8.82
CHEMBL1801562 — — 1 8.72
CHEMBL1801567 — — 1 8.59
CHEMBL1801855 — — 1 8.54
CHEMBL1801937 — — 1 8.44
CHEMBL1801861 — — 1 8.42
CHEMBL1801560 — — 1 8.38
CHEMBL1801559 — — 1 8.21
CHEMBL1801935 — — 1 7.96
CHEMBL1801860 — — 1 7.92
CHEMBL1801570 — — 1 7.92
CHEMBL1801565 — — 1 7.92
CHEMBL1801568 — — 1 7.89
CHEMBL1801556 — — 1 7.82
CHEMBL1801936 — — 1 7.60
CHEMBL1801870 — — 1 7.54
CHEMBL1801550 — — 1 7.52
CHEMBL1801553 — — 1 7.51
CHEMBL1801941 — — 1 7.47
CHEMBL1801933 — — 1 7.40
CHEMBL1801547 — — 1 7.31
CHEMBL1801569 — — 1 7.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1801863 — IC50 = 0.3 nM 9.52
CHEMBL123756 — IC50 = 0.31 nM 9.51
CHEMBL1801864 — IC50 = 0.45 nM 9.35
CHEMBL1801934 — IC50 = 0.55 nM 9.26
CHEMBL1801862 — IC50 = 0.79 nM 9.10
CHEMBL1801566 — IC50 = 1.2 nM 8.92
CHEMBL1801561 — IC50 = 1.3 nM 8.89
CHEMBL1801552 — IC50 = 1.4 nM 8.85
CHEMBL1801563 — IC50 = 1.5 nM 8.82
CHEMBL1801562 — IC50 = 1.9 nM 8.72
CHEMBL1801567 — IC50 = 2.6 nM 8.59
CHEMBL1801855 — IC50 = 2.9 nM 8.54
CHEMBL1801937 — IC50 = 3.6 nM 8.44
CHEMBL1801861 — IC50 = 3.8 nM 8.42
CHEMBL1801560 — IC50 = 4.2 nM 8.38
CHEMBL1801559 — IC50 = 6.1 nM 8.21
CHEMBL1801935 — IC50 = 11.0 nM 7.96
CHEMBL1801860 — IC50 = 12.0 nM 7.92
CHEMBL1801570 — IC50 = 12.0 nM 7.92
CHEMBL1801565 — IC50 = 12.0 nM 7.92
CHEMBL1801568 — IC50 = 13.0 nM 7.89
CHEMBL1801556 — IC50 = 15.0 nM 7.82
CHEMBL1801936 — IC50 = 25.0 nM 7.60
CHEMBL1801870 — IC50 = 29.0 nM 7.54
CHEMBL1801550 — IC50 = 30.0 nM 7.52
CHEMBL1801553 — IC50 = 31.0 nM 7.51
CHEMBL1801941 — IC50 = 34.0 nM 7.47
CHEMBL1801933 — IC50 = 40.0 nM 7.40
CHEMBL1801547 — IC50 = 49.0 nM 7.31
CHEMBL1801569 — IC50 = 56.0 nM 7.25
CHEMBL1801940 — IC50 = 85.0 nM 7.07
CHEMBL1801867 — IC50 = 90.0 nM 7.05
CHEMBL1801548 — IC50 = 98.0 nM 7.01
CHEMBL1801564 — IC50 = 110.0 nM 6.96
CHEMBL1801938 — IC50 = 130.0 nM 6.89
CHEMBL1801549 — IC50 = 150.0 nM 6.82
CHEMBL1801854 — IC50 = 210.0 nM 6.68
CHEMBL1801551 — IC50 = 250.0 nM 6.60
CHEMBL1801555 — IC50 = 330.0 nM 6.48
CHEMBL1801558 — IC50 = 420.0 nM 6.38
CHEMBL1801869 — IC50 = 600.0 nM 6.22
CHEMBL1801571 — IC50 = 660.0 nM 6.18
CHEMBL1801856 — IC50 = 950.0 nM 6.02
CHEMBL1801866 — IC50 = 1200.0 nM 5.92
CHEMBL1801857 — IC50 = 2600.0 nM 5.58
CHEMBL1801865 — IC50 = 2800.0 nM 5.55
CHEMBL1801871 — IC50 = 7200.0 nM 5.14
CHEMBL1801859 — IC50 > 10000.0 nM -
CHEMBL1801858 — IC50 > 10000.0 nM -
CHEMBL1801868 — IC50 > 10000.0 nM -