Assay Detail

CHEMBL4676718

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Binding

Inhibition of PARP3 (unknown origin)

ChEMBL ↗

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Target

Protein mono-ADP-ribosyltransferase PARP3 (CHEMBL5083) ↗

Open DB target context

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Protein mono-ADP-ribosyltransferase PARP3 (CHEMBL5083) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Protein mono-ADP-ribosyltransferase PARP3

CHEMBL5083

Anchored from Assay target.

Protein identity Protein mono-ADP-ribosyltransferase PARP3

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

Target

Protein mono-ADP-ribosyltransferase PARP3 (CHEMBL5083) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of isoquinolinone and naphthyridinone-based inhibitors of poly(ADP-ribose) polymerase-1 (PARP1) as anticancer agents: Structure activity relationship and preclinical characterization.

Karche NP,Bhonde M,Sinha N,Jana G,Kukreja G,Kurhade SP,Jagdale AR,Tilekar AR,Hajare AK,Jadhav GR,Gupta NR,Limaye R,Khedkar N,Thube BR,Shaikh JS,Rao Irlapati N,Phukan S,Gole G,Bommakanti A,Khanwalkar H,Pawar Y,Kale R,Kumar R,Gupta R,Praveen Kumar VR,Wahid S,Francis A,Bhat T,Kamble N,Patil V,Nigade PB,Modi D,Pawar S,Naidu S,Volam H,Pagdala V,Mallurwar S,Goyal H,Bora P,Ahirrao P,Singh M,Kamalakannan P,Naik KR,Kumar P,Powar RG,Shankar RB,Bernstein PR,Gundu J,Nemmani K,Narasimham L,George KS,Sharma S,Bakhle D,Kamboj RK,Palle VP
Bioorg Med Chem (2020) 28 : 115819 -115819
PubMed 33120078 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	5.10	5.10

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4776820	—	—	1	5.10

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4776820	—	IC50	=	8000.0	nM	5.10