DGIdb - CHEK1 Gene Record

CHEK1 1111 Druggable GenomeClinically Actionable

Alternate Names:

1111
CHECKPOINT KINASE 1
CHEK1
CHK1
603078
1925
ENSG00000149554
OTTHUMG00000165853
O14757
Cell cycle checkpoint kinase
CHK1 checkpoint homolog
Serine/threonine-protein kinase Chk1
Checkpoint kinase-1
SERINE/THREONINE-PROTEIN KINASE CHK1 (EC 2.7.1.37). [SOURCE:UNIPROT/SWISSPROT;ACC:O14757]
CHK1_HUMAN
981
T62449

Gene Info:

Target Class	Enzymes
Target Subclass	EC:2.7.11.1
Human Readable Name	DRUGGABLE GENOME
Uniprot Status	Swiss-Prot
Human Readable Name	KINASE
Interpro Name	Serine/threonine- / dual-specificity protein kinase, catalytic domain
Uniprot Evidence	1: Evidence at protein level
Interpro Type	Domain
Interpro Short Name	Ser/Thr_dual-sp_kinase_dom
Interpro Acc	IPR002290
Gene Biotype	PROTEIN_CODING

(15 More Sources)

Gene Categories: Category Details

DNA REPAIR
KINASE
SERINE THREONINE KINASE
DRUGGABLE GENOME
CLINICALLY ACTIONABLE
TRANSCRIPTION FACTOR

Publications:

Roy RV et al., 2013, Withaferin A, a steroidal lactone from Withania somnifera, induces mitotic catastrophe and growth arrest in prostate cancer cells., J Nat Prod
Sen et al., 2017, CHK1 Inhibition in Small-Cell Lung Cancer Produces Single-Agent Activity in Biomarker-Defined Disease Subsets and Combination Activity with Cisplatin or Olaparib., Cancer Res.
Zhao et al., 2002, Structural basis for Chk1 inhibition by UCN-01., J. Biol. Chem.
Ho et al., 2005, The relative contribution of CHK1 and CHK2 to Adriamycin-induced checkpoint., Exp. Cell Res.
Matthews et al., 2007, Pharmacological abrogation of S-phase checkpoint enhances the anti-tumor activity of gemcitabine in vivo., Cell Cycle
Lainchbury M et al., 2012, Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors., J Med Chem
Kamal A et al., 2012, Synthesis and biological evaluation of 4β-sulphonamido and 4β-[(4'-sulphonamido)benzamide]podophyllotoxins as DNA topoisomerase-IIα and apoptosis inducing agents., Bioorg Med Chem
Rodriguez et al., 2006, Chk1 and p21 cooperate to prevent apoptosis during DNA replication fork stress., Mol. Biol. Cell
Kennedy DR et al., 2007, Designer enediynes generate DNA breaks, interstrand cross-links, or both, with concomitant changes in the regulation of DNA damage responses., Proc Natl Acad Sci U S A

CHEMBL506048 CHEK1

Interaction Score: 3.75

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17978180

Sources:
DTC
CHEMBL2203843 CHEK1

Interaction Score: 3.75

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
23082860

Sources:
DTC
SCH-900776 CHEK1

Interaction Score: 3.75

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase Chk1 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
RG-7741 CHEK1

Interaction Score: 1.87

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase Chk1 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
RG-7602 CHEK1

Interaction Score: 1.87

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase Chk1 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
RABUSERTIB CHEK1

Interaction Score: 1.87

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase Chk1 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
AZD-7762 CHEK1

Interaction Score: 1.87

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase Chk1 inhibitor

Direct Interaction yes

Notes

PMIDs:
None found

Sources:
TALC ChemblInteractions TTD
PREXASERTIB CHEK1

Interaction Score: 1.87

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase Chk1 inhibitor

Direct Interaction yes

PMIDs:
28490518

Sources:
ChemblInteractions CIViC
LY-2606368 CHEK1

Interaction Score: 1.87

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serine/threonine-protein kinase Chk1 inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
XL-844 CHEK1

Interaction Score: 0.94

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase Chk1 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
THYMIDINE CHEK1

Interaction Score: 0.75

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16280359

Sources:
NCI
UCN-01 CHEK1

Interaction Score: 0.37

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase Chk1 inhibitor

Direct Interaction yes

PMIDs:
12244092

Sources:
ChemblInteractions NCI TTD
PF-00477736 CHEK1

Interaction Score: 0.31

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase Chk1 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
WITHAFERIN A CHEK1

Interaction Score: 0.31

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24079846

Sources:
DTC
DIMETHYLADENINE CHEK1

Interaction Score: 0.21

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ADRIAMYCIN CHEK1

Interaction Score: 0.2

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15707569

Sources:
NCI
OLAPARIB CHEK1

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
28490518

Sources:
CIViC
CI-1040 CHEK1

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CHEMBL578061 CHEK1

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ETOPOSIDE CHEK1

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22364746

Sources:
DTC
GEMCITABINE CHEK1

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17245119

Sources:
NCI
CHEMBL1997335 CHEK1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DACTOLISIB CHEK1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PALBOCICLIB CHEK1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
KENPAULLONE CHEK1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CISPLATIN CHEK1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
28490518

Sources:
CIViC
R-406 CHEK1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
RG-1530 CHEK1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB CHEK1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
SP-600125 CHEK1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CYC-116 CHEK1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TAE-684 CHEK1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CENISERTIB CHEK1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

Ensembl: ENSG00000149554
- Version: 101_38
Alternate Names:

CHEK1 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
HopkinsGroom: O14757
- Version: 11-September-2012
Alternate Names:

O14757 Uniprot Accession

ENSG00000149554 Ensembl Gene Id

CHK1_HUMAN Uniprot Id

Gene Info:

Uniprot Status Swiss-Prot

Human Readable Name KINASE

Interpro Name Serine/threonine- / dual-specificity protein kinase, catalytic domain

Gene Categories:

KINASE, DRUGGABLE GENOME

Publications:
TdgClinicalTrial: O14757
- Version: January-2014
Alternate Names:

CHEK1 Gene Symbol

Gene Info:

Target Class Enzymes

Target Subclass EC:2.7.11.1

Publications:
RussLampel: ENSG00000149554
- Version: 26-July-2011
Alternate Names:

CHEK1 Display Id

SERINE/THREONINE-PROTEIN KINASE CHK1 (EC 2.7.1.37). [SOURCE:UNIPROT/SWISSPROT;ACC:O14757] Description

ENSG00000149554 Ensembl Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:

CIViC: CHEK1

Version: 14-September-2020

Alternate Names:

1111 Entrez Gene ID

981 CIViC Gene ID

Gene Info:

Publications:

Sen et al., 2017, CHK1 Inhibition in Small-Cell Lung Cancer Produces Single-Agent Activity in Biomarker-Defined Disease Subsets and Combination Activity with Cisplatin or Olaparib., Cancer Res.

TTD: Checkpoint kinase-1
- Version: 2020.06.01
Alternate Names:

CHK1 TTD Gene Abbreviation

T62449 TTD Target ID

Gene Info:

Publications:

Matthews TP et al., 2013, Structure-based design, discovery and development of checkpoint kinase inhibitors as potential anticancer therapies., Expert Opin Drug Discov

NCI: CHEK1

Version: 14-September-2017

Alternate Names:

Gene Info:

Publications:

Zhao et al., 2002, Structural basis for Chk1 inhibition by UCN-01., J. Biol. Chem.

Matthews et al., 2007, Pharmacological abrogation of S-phase checkpoint enhances the anti-tumor activity of gemcitabine in vivo., Cell Cycle

Ho et al., 2005, The relative contribution of CHK1 and CHK2 to Adriamycin-induced checkpoint., Exp. Cell Res.

DTC: CHEK1

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

Kennedy DR et al., 2007, Designer enediynes generate DNA breaks, interstrand cross-links, or both, with concomitant changes in the regulation of DNA damage responses., Proc Natl Acad Sci U S A

Roy RV et al., 2013, Withaferin A, a steroidal lactone from Withania somnifera, induces mitotic catastrophe and growth arrest in prostate cancer cells., J Nat Prod

Lainchbury M et al., 2012, Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors., J Med Chem

TALC: CHK1
- Version: 12-May-2016
Alternate Names:

CHK1 Gene Symbol

Gene Info:

Publications:
HingoraniCasas: ENSG00000149554
- Version: 31-May-2017
Alternate Names:

ENSG00000149554 Gene Symbol

CHEK1 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
ChemblInteractions: CHK1
- Version: chembl_23
Alternate Names:

CHK1 GENE_SYMBOL

CHEK1 GENE_SYMBOL

Serine/threonine-protein kinase Chk1 UNIPROT

Gene Info:

Publications:
GO: CHEK1
- Version: 01-February-2022
Alternate Names:

CHK1 GO Gene Synonym

Gene Info:

Gene Categories:

DNA REPAIR, SERINE THREONINE KINASE

Publications:
Tempus: CHEK1
- Version: 11-November-2018
Alternate Names:

CHEK1 Gene Symbol

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
dGene: CHEK1
- Version: 27-Jun-2013
Alternate Names:

1111 Gene ID

CHK1 dGene Synonym

Gene Info:

Gene Categories:

KINASE, SERINE THREONINE KINASE

Publications:
Pharos: CHEK1
- Version: 01-February-2022
Alternate Names:

Serine/threonine-protein kinase Chk1 Gene Name

O14757 UniProt ID

Gene Info:

Gene Categories:

KINASE, TRANSCRIPTION FACTOR

Publications:
MskImpact: CHEK1
- Version: May-2015
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
FoundationOneGenes: CHEK1
- Version: 03-September-2020
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
CarisMolecularIntelligence: CHEK1
- Version: 04-September-2020
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
Oncomine: CHEK1
- Version: v3
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:

Mechanism of Interaction	Serine/threonine-protein kinase Chk1 inhibitor
Direct Interaction	yes

O14757	Uniprot Accession
ENSG00000149554	Ensembl Gene Id
CHK1_HUMAN	Uniprot Id

CHEK1	Display Id
SERINE/THREONINE-PROTEIN KINASE CHK1 (EC 2.7.1.37). [SOURCE:UNIPROT/SWISSPROT;ACC:O14757]	Description
ENSG00000149554	Ensembl Gene Id

CHK1	GENE_SYMBOL
CHEK1	GENE_SYMBOL
Serine/threonine-protein kinase Chk1	UNIPROT

Serine/threonine-protein kinase Chk1	Gene Name
O14757	UniProt ID

CHEK1 Gene Record

CHEK1 1111 Druggable GenomeClinically Actionable

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 17978180

Sources: DTC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 23082860

Sources: DTC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Serine/threonine-protein kinase Chk1 inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Serine/threonine-protein kinase Chk1 inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Serine/threonine-protein kinase Chk1 inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Serine/threonine-protein kinase Chk1 inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Serine/threonine-protein kinase Chk1 inhibitor Direct Interaction yes Notes

PMIDs: None found

Sources: TALC ChemblInteractions TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Serine/threonine-protein kinase Chk1 inhibitor Direct Interaction yes

PMIDs: 28490518

Sources: ChemblInteractions CIViC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Serine/threonine-protein kinase Chk1 inhibitor

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Serine/threonine-protein kinase Chk1 inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16280359

Sources: NCI

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Serine/threonine-protein kinase Chk1 inhibitor Direct Interaction yes

PMIDs: 12244092

Sources: ChemblInteractions NCI TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Serine/threonine-protein kinase Chk1 inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24079846

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15707569

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 28490518

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

Interaction Types & Directionality:

n/a

PMIDs:
17978180

Sources:
DTC

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
23082860

Sources:
DTC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase Chk1 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase Chk1 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase Chk1 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase Chk1 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase Chk1 inhibitor

Direct Interaction yes

Notes

PMIDs:
None found

Sources:
TALC ChemblInteractions TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase Chk1 inhibitor

Direct Interaction yes

PMIDs:
28490518

Sources:
ChemblInteractions CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serine/threonine-protein kinase Chk1 inhibitor

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase Chk1 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
16280359

Sources:
NCI

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase Chk1 inhibitor

Direct Interaction yes

PMIDs:
12244092

Sources:
ChemblInteractions NCI TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Serine/threonine-protein kinase Chk1 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
24079846

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
15707569

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
28490518

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
22364746

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
17245119

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a