Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL829484

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

Binding
Inhibitory concentration against human poly (ADP-ribose) polymerase 1 (PARP-1)
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Phthalazinones. Part 1: The design and synthesis of a novel series of potent inhibitors of poly(ADP-ribose)polymerase.
Loh VM, Cockcroft XL, Dillon KJ, Dixon L, Drzewiecki J, Eversley PJ, Gomez S, Hoare J, Kerrigan F, Matthews IT, Menear KA, Martin NM, Newton RF, Paul J, Smith GC, Vile J, Whittle AJ.
Bioorg Med Chem Lett (2005) 15 : 2235 -2238
PubMed 15837300 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 7.44 8.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL370838 1 8.42
CHEMBL370217 1 8.39
CHEMBL436298 1 8.30
CHEMBL196444 1 8.30
CHEMBL196450 1 8.17
CHEMBL195966 1 8.02
CHEMBL197192 1 8.01
CHEMBL382950 1 8.00
CHEMBL195402 1 7.92
CHEMBL195464 1 7.89
CHEMBL363617 1 7.89
CHEMBL195913 1 7.72
CHEMBL371425 1 7.70
CHEMBL383578 1 7.57
CHEMBL371205 1 7.48
CHEMBL371244 1 7.44
CHEMBL193903 1 7.33
CHEMBL381208 1 7.30
CHEMBL196507 1 7.26
CHEMBL372450 1 7.25
CHEMBL425560 1 7.05
CHEMBL381652 1 7.05
CHEMBL193638 1 6.94
CHEMBL196559 1 6.92
CHEMBL370692 1 6.75
CHEMBL193918 1 6.72
CHEMBL193917 1 6.54
CHEMBL193512 1 6.43
CHEMBL196883 1 6.27
CHEMBL66761 1 6.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL370838 IC50 = 3.8 nM 8.42
CHEMBL370217 IC50 = 4.1 nM 8.39
CHEMBL436298 IC50 = 5.0 nM 8.30
CHEMBL196444 IC50 = 5.0 nM 8.30
CHEMBL196450 IC50 = 6.8 nM 8.17
CHEMBL195966 IC50 = 9.5 nM 8.02
CHEMBL197192 IC50 = 9.8 nM 8.01
CHEMBL382950 IC50 = 10.0 nM 8.00
CHEMBL195402 IC50 = 12.0 nM 7.92
CHEMBL195464 IC50 = 13.0 nM 7.89
CHEMBL363617 IC50 = 13.0 nM 7.89
CHEMBL195913 IC50 = 19.0 nM 7.72
CHEMBL371425 IC50 = 20.0 nM 7.70
CHEMBL383578 IC50 = 27.0 nM 7.57
CHEMBL371205 IC50 = 33.0 nM 7.48
CHEMBL371244 IC50 = 36.0 nM 7.44
CHEMBL193903 IC50 = 47.0 nM 7.33
CHEMBL381208 IC50 = 50.0 nM 7.30
CHEMBL196507 IC50 = 55.0 nM 7.26
CHEMBL372450 IC50 = 56.0 nM 7.25
CHEMBL425560 IC50 = 90.0 nM 7.05
CHEMBL381652 IC50 = 90.0 nM 7.05
CHEMBL193638 IC50 = 116.0 nM 6.94
CHEMBL196559 IC50 = 120.0 nM 6.92
CHEMBL370692 IC50 = 180.0 nM 6.75
CHEMBL193918 IC50 = 189.0 nM 6.72
CHEMBL193917 IC50 = 290.0 nM 6.54
CHEMBL193512 IC50 = 370.0 nM 6.43
CHEMBL196883 IC50 = 540.0 nM 6.27
CHEMBL66761 IC50 = 770.0 nM 6.11