POLY (ADP-RIBOSE) POLYMERASE 1

Investigational

Approval Year

Substance Class	Protein Created by `admin` on `Tue Apr 01 19:47:14 GMT 2025` Edited by `admin` on `Tue Apr 01 19:47:14 GMT 2025`
Protein Sub Type
Sequence Type	COMPLETE
Record UNII	U25G2OFC53
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

POLY (ADP-RIBOSE) POLYMERASE 1

Common Name

English

ADP-RIBOSYLTRANSFERASE DIPHTHERIA TOXIN-LIKE 1

Preferred Name

English

PARP-1

Common Name

English

PARP1

Common Name

English

NAD(+) ADP-RIBOSYLTRANSFERASE 1

Common Name

English

POLY(ADP-RIBOSE) SYNTHASE 1

Common Name

English

Code System Code Type Description

FDA UNII

U25G2OFC53

Created by admin on Tue Apr 01 19:47:14 GMT 2025 , Edited by admin on Tue Apr 01 19:47:14 GMT 2025

PRIMARY

UNIPROT

P09874

Created by admin on Tue Apr 01 19:47:14 GMT 2025 , Edited by admin on Tue Apr 01 19:47:14 GMT 2025

PRIMARY

WIKIPEDIA

PARP1

Created by admin on Tue Apr 01 19:47:14 GMT 2025 , Edited by admin on Tue Apr 01 19:47:14 GMT 2025

PRIMARY

Linkage Type	Residue Index
ZINC FINGER	1_112	1_202
ZINC FINGER	1_8	1_92

Related Record Type Details


					9X5A2QIA7C

2X-121

INHIBITOR -> TARGET


					PUP792O0IW

VENADAPARIB

INHIBITOR -> TARGET

Amount:


					01O4K0631N

VELIPARIB

INHIBITOR -> TARGET


					3K288XF5XJ

AZD-2461

INHIBITOR -> TARGET


					TWF0ML1CK8

FUZULOPARIB

INHIBITOR -> TARGET

Comments:

Fluzoparib was well ordered in the catalytic active site of PARP1 with the same binding mode as olaparib.

Qualification:

IC50

Amount:


					9TSU9SA6UZ

NMS-P118

INHIBITOR -> TARGET

Comments:

exceedingly selective PARP-1 inhibitor, whose unprecedented selectivity might reside in its distinct binding poses within the catalytic domains of PARP-1

Qualification:

Kd

Amount:


					MNZ4OP95CF

SENAPARIB

INHIBITOR -> TARGET


					9NN2OZ1YX4

MEFUPARIB

INHIBITOR -> TARGET

Comments:

The selective inhibition of MPH against PARPs analyzed by biotinylated NAD+ -based luminescence assays

Qualification:

IC50

Amount:


					U6N7333GDW

NESUPARIB

INHIBITOR -> TARGET

Comments:

Selective for PARP-1 over PARP-2

Qualification:

IC50

Amount:


					9UG32UQW48

Palacaparib

INHIBITOR -> TARGET

Comments:

poly (ADP-ribose) polymerase (PARP) inhibitor, antineoplastic

Amount:


					16MZ1V3RBT

Saruparib

INHIBITOR -> TARGET

Amount:


					R252S84C2I

AMELPARIB

INHIBITOR -> TARGET


					1RW94540W6

3-[2-[(2R)-2-(Hydroxymethyl)-1-pyrrolidinyl]ethyl]-5-methyl-1(2H)-isoquinolinone

INHIBITOR -> TARGET

Amount:


					8375F9S90C

PAMIPARIB

INHIBITOR -> TARGET

Qualification:

IC50

Amount:


					343SLZ0F89

INO-1001 FREE BASE

INHIBITOR -> TARGET


					WOH1JD9AR8

Olaparib

INHIBITOR -> TARGET

Comments:

DT40 cells cytotoxicity

Interaction Type:

BINDING

Qualification:

IC50

Amount:


					9B8U3WZ84W

FLUORTHANATRACE F-18

RADIOLIGAND->TARGET

Amount:


					WOH1JD9AR8

Olaparib

INHIBITOR -> TARGET

Interaction Type:

BINDING

Qualification:

EC50

Amount:


					ZMX54372EH

OLAPARIB-BODIPY FL

INHIBITOR -> TARGET


					S4XZG5Q57F

Veliparib lactam metabolite

INHIBITOR -> TARGET

Comments:

5 fold less active than Veliparib in-vitro and 14 fold less active it cell assay.

Amount:

Structural Modifications

Modification Type	Location Site	Location Type	Residue Modified	Extent	Fragment Name	Fragment Approval
AMINO ACID SUBSTITUTION	[1_96] [1_104] [1_130] [1_599] [1_620]		LYSINE	Amount:	N6-ACETYLLYSINE	470AD5VY1X
AMINO ACID SUBSTITUTION	[1_1]		ALANINE	Amount:	N-ACETYLALANINE	26C4VY6Z0M

Name	Property Type	Amount	Referenced Substance	Defining	Parameters	References
MOL_WEIGHT	CHEMICAL