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Assay Detail

CHEMBL4410833

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Functional
Antiproliferative activity against human A2780 cells incubated for 72 hrs by CellTiterGlo assay
29
Total Activities
28
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

Scaffold Morphing Identifies 3-Pyridyl Azetidine Ureas as Inhibitors of Nicotinamide Phosphoribosyltransferase (NAMPT).
Palacios DS, Meredith EL, Kawanami T, Adams CM, Chen X, Darsigny V, Palermo M, Baird D, George EL, Guy C, Hewett J, Tierney L, Thigale S, Wang L, Weihofen WA.
ACS Med Chem Lett (2019) 10 : 1524 -1529
PubMed 31749905 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 7.72 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4558559 1 9.70
CHEMBL4438525 1 9.40
CHEMBL4536277 1 9.22
CHEMBL4450629 1 9.15
CHEMBL4446132 1 9.05
CHEMBL4483695 1 8.82
CHEMBL4448916 1 8.64
CHEMBL4546918 1 8.30
CHEMBL4456070 1 8.24
CHEMBL4556614 1 8.23
CHEMBL4561577 1 8.12
CHEMBL4457730 1 7.96
CHEMBL4586676 1 7.77
CHEMBL4451769 1 7.60
CHEMBL4205098 1 7.57
CHEMBL4439536 1 7.47
CHEMBL4532502 1 7.44
CHEMBL4469631 1 7.35
CHEMBL4441045 1 7.34
CHEMBL4571655 1 7.24
CHEMBL4575553 1 7.17
CHEMBL4213004 1 7.00
CHEMBL4444464 1 6.62
CHEMBL4552727 1 6.47
CHEMBL4540185 1 6.30
CHEMBL4541056 1 6.11
CHEMBL4561390 1 5.99
CHEMBL4446579 2 5.99

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4558559 IC50 = 0.2 nM 9.70
CHEMBL4438525 IC50 = 0.4 nM 9.40
CHEMBL4536277 IC50 = 0.6 nM 9.22
CHEMBL4450629 IC50 = 0.7 nM 9.15
CHEMBL4446132 IC50 = 0.9 nM 9.05
CHEMBL4483695 IC50 = 1.5 nM 8.82
CHEMBL4448916 IC50 = 2.3 nM 8.64
CHEMBL4546918 IC50 = 5.0 nM 8.30
CHEMBL4456070 IC50 = 5.7 nM 8.24
CHEMBL4556614 IC50 = 5.9 nM 8.23
CHEMBL4561577 IC50 = 7.6 nM 8.12
CHEMBL4457730 IC50 = 11.0 nM 7.96
CHEMBL4586676 IC50 = 17.0 nM 7.77
CHEMBL4451769 IC50 = 25.0 nM 7.60
CHEMBL4205098 IC50 = 27.0 nM 7.57
CHEMBL4439536 IC50 = 34.0 nM 7.47
CHEMBL4532502 IC50 = 36.0 nM 7.44
CHEMBL4469631 IC50 = 45.0 nM 7.35
CHEMBL4441045 IC50 = 46.0 nM 7.34
CHEMBL4571655 IC50 = 58.0 nM 7.24
CHEMBL4575553 IC50 = 68.0 nM 7.17
CHEMBL4213004 IC50 = 100.0 nM 7.00
CHEMBL4444464 IC50 = 240.0 nM 6.62
CHEMBL4552727 IC50 = 340.0 nM 6.47
CHEMBL4540185 IC50 = 500.0 nM 6.30
CHEMBL4541056 IC50 = 770.0 nM 6.11
CHEMBL4561390 IC50 = 1030.0 nM 5.99
CHEMBL4446579 IC50 = 1030.0 nM 5.99
CHEMBL4446579 IC50 > 2500.0 nM -