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Assay Detail

CHEMBL4036656

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

Functional
Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 5 days by Cell-titer Glo reagent based assay
48
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type PC-3
Confidence 1 — Organism
Curated By Autocuration

Target

PC-3 (CHEMBL390)
Type CELL-LINE
Organism Homo sapiens

Publication

SAR and characterization of non-substrate isoindoline urea inhibitors of nicotinamide phosphoribosyltransferase (NAMPT).
Curtin ML, Heyman HR, Clark RF, Sorensen BK, Doherty GA, Hansen TM, Frey RR, Sarris KA, Aguirre AL, Shrestha A, Tu N, Woller K, Pliushchev MA, Sweis RF, Cheng M, Wilsbacher JL, Kovar PJ, Guo J, Cheng D, Longenecker KL, Raich D, Korepanova AV, Soni NB, Algire MA, Richardson PL, Marin VL, Badagnani I, Vasudevan A, Buchanan FG, Maag D, Chiang GG, Tse C, Michaelides MR.
Bioorg Med Chem Lett (2017) 27 : 3317 -3325
PubMed 28610984 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 48 7.58 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3913732 1 8.85
CHEMBL4060799 1 8.64
CHEMBL3943749 1 8.55
CHEMBL4089003 1 8.49
CHEMBL4096471 1 8.41
CHEMBL17289 CHS-828 1.0 1 8.36
CHEMBL4077485 1 8.25
CHEMBL566757 DAPORINAD 2.0 1 8.24
CHEMBL4076064 1 8.19
CHEMBL3926822 1 8.19
CHEMBL4105475 1 8.18
CHEMBL4083505 1 8.10
CHEMBL3922276 1 8.09
CHEMBL3908312 1 8.08
CHEMBL3960317 1 8.08
CHEMBL3941284 1 8.00
CHEMBL3984857 1 7.85
CHEMBL4086819 1 7.82
CHEMBL4077254 1 7.77
CHEMBL3904786 1 7.77
CHEMBL3896390 1 7.75
CHEMBL4062838 1 7.72
CHEMBL3892230 1 7.68
CHEMBL3938019 1 7.68
CHEMBL4082366 1 7.62
CHEMBL4076641 1 7.52
CHEMBL3940058 1 7.50
CHEMBL3950120 1 7.42
CHEMBL3975643 1 7.32
CHEMBL3929298 1 7.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3913732 IC50 = 1.4 nM 8.85
CHEMBL4060799 IC50 = 2.3 nM 8.64
CHEMBL3943749 IC50 = 2.8 nM 8.55
CHEMBL4089003 IC50 = 3.2 nM 8.49
CHEMBL4096471 IC50 = 3.9 nM 8.41
CHEMBL17289 CHS-828 IC50 = 4.4 nM 8.36
CHEMBL4077485 IC50 = 5.6 nM 8.25
CHEMBL566757 DAPORINAD IC50 = 5.7 nM 8.24
CHEMBL4076064 IC50 = 6.5 nM 8.19
CHEMBL3926822 IC50 = 6.5 nM 8.19
CHEMBL4105475 IC50 = 6.6 nM 8.18
CHEMBL4083505 IC50 = 7.9 nM 8.10
CHEMBL3922276 IC50 = 8.1 nM 8.09
CHEMBL3908312 IC50 = 8.4 nM 8.08
CHEMBL3960317 IC50 = 8.4 nM 8.08
CHEMBL3941284 IC50 = 10.0 nM 8.00
CHEMBL3984857 IC50 = 14.0 nM 7.85
CHEMBL4086819 IC50 = 15.0 nM 7.82
CHEMBL4077254 IC50 = 17.0 nM 7.77
CHEMBL3904786 IC50 = 17.0 nM 7.77
CHEMBL3896390 IC50 = 18.0 nM 7.75
CHEMBL4062838 IC50 = 19.0 nM 7.72
CHEMBL3892230 IC50 = 21.0 nM 7.68
CHEMBL3938019 IC50 = 21.0 nM 7.68
CHEMBL4082366 IC50 = 24.0 nM 7.62
CHEMBL4076641 IC50 = 30.0 nM 7.52
CHEMBL3940058 IC50 = 32.0 nM 7.50
CHEMBL3950120 IC50 = 38.0 nM 7.42
CHEMBL3975643 IC50 = 48.0 nM 7.32
CHEMBL3929298 IC50 = 56.0 nM 7.25
CHEMBL3899179 IC50 = 66.0 nM 7.18
CHEMBL3930840 IC50 = 68.0 nM 7.17
CHEMBL3974537 IC50 = 68.0 nM 7.17
CHEMBL3907814 IC50 = 84.0 nM 7.08
CHEMBL3953911 IC50 = 640.0 nM 6.19
CHEMBL3918436 IC50 = 730.0 nM 6.14
CHEMBL3937583 IC50 = 880.0 nM 6.06
CHEMBL4099778 IC50 = 1100.0 nM 5.96
CHEMBL4081887 IC50 = 2300.0 nM 5.64
CHEMBL3890237 IC50 = 8000.0 nM 5.10
CHEMBL3949149 IC50 > 10000.0 nM -
CHEMBL3715249 IC50 > 10000.0 nM -
CHEMBL3972460 IC50 > 10000.0 nM -
CHEMBL3890168 IC50 > 10000.0 nM -
CHEMBL3925932 IC50 > 10000.0 nM -
CHEMBL4062656 IC50 > 10000.0 nM -
CHEMBL2419508 IC50 > 10000.0 nM -
CHEMBL4090863 IC50 > 12500.0 nM -