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Assay Detail

CHEMBL3607346

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

Binding
Binding affinity to full length recombinant human PARP-1 by fluorescence polarization displacement assay
ChEMBL ↗
59
Total Activities
59
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy.
Papeo G, Posteri H, Borghi D, Busel AA, Caprera F, Casale E, Ciomei M, Cirla A, Corti E, D'Anello M, Fasolini M, Forte B, Galvani A, Isacchi A, Khvat A, Krasavin MY, Lupi R, Orsini P, Perego R, Pesenti E, Pezzetta D, Rainoldi S, Riccardi-Sirtori F, Scolaro A, Sola F, Zuccotto F, Felder ER, Donati D, Montagnoli A.
J Med Chem (2015) 58 : 6875 -6898
PubMed 26222319 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 59 6.98 7.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3605984 — — 1 7.51
CHEMBL3605972 — — 1 7.50
CHEMBL3605973 — — 1 7.48
CHEMBL3606015 — — 1 7.47
CHEMBL3605999 — — 1 7.47
CHEMBL3605976 — — 1 7.46
CHEMBL3606005 — — 1 7.41
CHEMBL3606008 — — 1 7.38
CHEMBL3605996 — — 1 7.38
CHEMBL3606003 — — 1 7.34
CHEMBL3605981 — — 1 7.31
CHEMBL3606014 — — 1 7.30
CHEMBL3605986 — — 1 7.30
CHEMBL3606006 — — 1 7.30
CHEMBL3606000 — — 1 7.28
CHEMBL3606004 — — 1 7.27
CHEMBL3605982 — — 1 7.25
CHEMBL3606007 — — 1 7.14
CHEMBL3606022 — — 1 7.10
CHEMBL1329044 — — 1 7.08
CHEMBL3605967 — — 1 7.06
CHEMBL3605970 — — 1 7.05
CHEMBL3605995 — — 1 6.95
CHEMBL3606019 — — 1 6.88
CHEMBL3605988 — — 1 6.82
CHEMBL3605975 — — 1 6.80
CHEMBL3605968 — — 1 6.66
CHEMBL3605987 — — 1 6.60
CHEMBL3605977 — — 1 6.54
CHEMBL3605971 — — 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3605984 — Kd = 31.0 nM 7.51
CHEMBL3605972 — Kd = 32.0 nM 7.50
CHEMBL3605973 — Kd = 33.0 nM 7.48
CHEMBL3606015 — Kd = 34.0 nM 7.47
CHEMBL3605999 — Kd = 34.0 nM 7.47
CHEMBL3605976 — Kd = 35.0 nM 7.46
CHEMBL3606005 — Kd = 39.0 nM 7.41
CHEMBL3606008 — Kd = 42.0 nM 7.38
CHEMBL3605996 — Kd = 42.0 nM 7.38
CHEMBL3606003 — Kd = 46.0 nM 7.34
CHEMBL3605981 — Kd = 49.0 nM 7.31
CHEMBL3606014 — Kd = 50.0 nM 7.30
CHEMBL3605986 — Kd = 50.0 nM 7.30
CHEMBL3606006 — Kd = 50.0 nM 7.30
CHEMBL3606000 — Kd = 53.0 nM 7.28
CHEMBL3606004 — Kd = 54.0 nM 7.27
CHEMBL3605982 — Kd = 56.0 nM 7.25
CHEMBL3606007 — Kd = 72.0 nM 7.14
CHEMBL3606022 — Kd = 80.0 nM 7.10
CHEMBL1329044 — Kd = 84.0 nM 7.08
CHEMBL3605967 — Kd = 87.0 nM 7.06
CHEMBL3605970 — Kd = 90.0 nM 7.05
CHEMBL3605995 — Kd = 113.0 nM 6.95
CHEMBL3606019 — Kd = 132.0 nM 6.88
CHEMBL3605988 — Kd = 150.0 nM 6.82
CHEMBL3605975 — Kd = 160.0 nM 6.80
CHEMBL3605968 — Kd = 220.0 nM 6.66
CHEMBL3605987 — Kd = 250.0 nM 6.60
CHEMBL3605977 — Kd = 290.0 nM 6.54
CHEMBL3605971 — Kd = 320.0 nM 6.50
CHEMBL3605979 — Kd = 330.0 nM 6.48
CHEMBL3605989 — Kd = 350.0 nM 6.46
CHEMBL3606002 — Kd = 410.0 nM 6.39
CHEMBL3605969 — Kd = 760.0 nM 6.12
CHEMBL3606020 — Kd = 1880.0 nM 5.73
CHEMBL3605980 — Kd = 2590.0 nM 5.59
CHEMBL3605994 — Kd < 30.0 nM -
CHEMBL3606013 — Kd < 30.0 nM -
CHEMBL3605997 — Kd < 30.0 nM -
CHEMBL3605998 — Kd < 30.0 nM -
CHEMBL3606001 — Kd < 30.0 nM -
CHEMBL3605974 — Kd < 30.0 nM -
CHEMBL3606023 — Kd < 30.0 nM -
CHEMBL3606021 — Kd < 30.0 nM -
CHEMBL3606024 — Kd < 30.0 nM -
CHEMBL3606012 — Kd < 30.0 nM -
CHEMBL3606011 — Kd < 30.0 nM -
CHEMBL3606010 — Kd < 30.0 nM -
CHEMBL3606009 — Kd < 30.0 nM -
CHEMBL3605978 — Kd < 30.0 nM -