Assay Detail

CHEMBL3607798

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Functional

Cytotoxicity against BRCA1-deficient human MDA-MB-436 cells assessed as inhibition of colony formation after 10 to 14 days by crystal violet staining

ChEMBL ↗

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Target

NON-PROTEIN TARGET (CHEMBL3879801) ↗

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NON-PROTEIN TARGET (CHEMBL3879801) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target NON-PROTEIN TARGET

CHEMBL3879801

Anchored from Assay target.

Protein identity NON-PROTEIN TARGET

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Functional
Organism	Homo sapiens
Cell Type	MDA-MB-436
Confidence	1 — Organism
Curated By	Autocuration

Target

NON-PROTEIN TARGET (CHEMBL3879801) ↗

Type	NON-MOLECULAR

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
IC50	2	6.54	6.85

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3606021	—	—	1	6.85
CHEMBL3606018	—	—	1	6.22

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3606021	—	IC50	=	140.0	nM	6.85
CHEMBL3606018	—	IC50	=	600.0	nM	6.22