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Assay Detail

CHEMBL761610

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Binding
Inhibitory activity against Poly (ADP-ribose) polymerase 1
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Poly [ADP-ribose] polymerase 1 (CHEMBL3105)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of poly ADP-ribose polymerase-1 inhibitors. 2. Biological evaluation of aza-5[H]-phenanthridin-6-ones as potent, aqueous-soluble compounds for the treatment of ischemic injuries.
Ferraris D, Ko YS, Pahutski T, Ficco RP, Serdyuk L, Alemu C, Bradford C, Chiou T, Hoover R, Huang S, Lautar S, Liang S, Lin Q, Lu MX, Mooney M, Morgan L, Qian Y, Tran S, Williams LR, Wu QY, Zhang J, Zou Y, Kalish V.
J Med Chem (2003) 46 : 3138 -3151
PubMed 12825952 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 6.63 7.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1160877 1 7.38
CHEMBL105995 1 7.35
CHEMBL107659 1 7.29
CHEMBL107284 1 7.24
CHEMBL108431 1 7.15
CHEMBL543394 1 7.12
CHEMBL558796 1 7.07
CHEMBL543157 1 7.01
CHEMBL543159 1 6.96
CHEMBL418813 1 6.95
CHEMBL320031 1 6.94
CHEMBL82342 1 6.89
CHEMBL542692 1 6.87
CHEMBL545507 1 6.85
CHEMBL542927 1 6.82
CHEMBL541576 1 6.78
CHEMBL311091 1 6.77
CHEMBL108106 1 6.76
CHEMBL106154 1 6.75
CHEMBL106734 1 6.68
CHEMBL106298 1 6.61
CHEMBL543393 1 6.56
CHEMBL110381 1 6.51
CHEMBL107709 1 6.47
CHEMBL45245 1 6.46
CHEMBL323384 1 6.11
CHEMBL108849 1 5.58
CHEMBL109064 1 5.54
CHEMBL107738 1 4.85
CHEMBL267373 BENZAMIDE 1 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1160877 IC50 = 42.0 nM 7.38
CHEMBL105995 IC50 = 45.0 nM 7.35
CHEMBL107659 IC50 = 51.0 nM 7.29
CHEMBL107284 IC50 = 58.0 nM 7.24
CHEMBL108431 IC50 = 71.0 nM 7.15
CHEMBL543394 IC50 = 75.0 nM 7.12
CHEMBL558796 IC50 = 86.0 nM 7.07
CHEMBL543157 IC50 = 98.0 nM 7.01
CHEMBL543159 IC50 = 111.0 nM 6.96
CHEMBL418813 IC50 = 112.0 nM 6.95
CHEMBL320031 IC50 = 116.0 nM 6.94
CHEMBL82342 IC50 = 128.0 nM 6.89
CHEMBL542692 IC50 = 134.0 nM 6.87
CHEMBL545507 IC50 = 142.0 nM 6.85
CHEMBL542927 IC50 = 150.0 nM 6.82
CHEMBL541576 IC50 = 165.0 nM 6.78
CHEMBL311091 IC50 = 169.0 nM 6.77
CHEMBL108106 IC50 = 173.0 nM 6.76
CHEMBL106154 IC50 = 180.0 nM 6.75
CHEMBL106734 IC50 = 209.0 nM 6.68
CHEMBL106298 IC50 = 247.0 nM 6.61
CHEMBL543393 IC50 = 277.0 nM 6.56
CHEMBL110381 IC50 = 311.0 nM 6.51
CHEMBL107709 IC50 = 339.0 nM 6.47
CHEMBL45245 IC50 = 350.0 nM 6.46
CHEMBL323384 IC50 = 774.0 nM 6.11
CHEMBL108849 IC50 = 2600.0 nM 5.58
CHEMBL109064 IC50 = 2900.0 nM 5.54
CHEMBL107738 IC50 = 14000.0 nM 4.85
CHEMBL267373 BENZAMIDE IC50 = 20000.0 nM 4.70
CHEMBL1140 NIACINAMIDE IC50 = 210000.0 nM -