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Target Report Card

Target Name and Classification

Target ID CHEMBL4630
Target Type SINGLE PROTEIN
Preferred Name Serine/threonine-protein kinase Chk1
Synonyms CHEK1 | CHK1 checkpoint homolog | CHK1 | Cell cycle checkpoint kinase | Checkpoint kinase-1 | Serine/threonine-protein kinase Chk1
Organism Homo sapiens
Species Group No
Protein Target Classification
  • enzyme > kinase > protein kinase > camk protein kinase group > camk protein kinase camk1 family > camk protein kinase chk1 subfamily

Target Components

Component Description Relationship Accession
Serine/threonine-protein kinase Chk1 SINGLE PROTEIN O14757

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL574737 (7S)-HYDROXYL-STAUROSPORINE Serine/threonine-protein kinase Chk1 inhibitor 2 Other PubMed PubMed
CHEMBL3039517 RABUSERTIB Serine/threonine-protein kinase Chk1 inhibitor 2 PubMed
CHEMBL3544911 PREXASERTIB Serine/threonine-protein kinase Chk1 inhibitor 2 PubMed
CHEMBL3545377 LY-2606368 Serine/threonine-protein kinase Chk1 inhibitor 2 Other PubMed
CHEMBL2041933 AZD-7762 Serine/threonine-protein kinase Chk1 inhibitor 1 Other PubMed PubMed
CHEMBL2386889 SCH-900776 Serine/threonine-protein kinase Chk1 inhibitor 1 PubMed
CHEMBL3544936 XL-844 Serine/threonine-protein kinase Chk1 inhibitor 1 Other PubMed PubMed
CHEMBL3545007 RG-7602 Serine/threonine-protein kinase Chk1 inhibitor 1 DOI
CHEMBL3545137 PF-00477736 Serine/threonine-protein kinase Chk1 inhibitor 1 PubMed PubMed
CHEMBL3545199 RG-7741 Serine/threonine-protein kinase Chk1 inhibitor 1 Other

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000149554
Ensembl ENSG00000149554
GO Cellular Component GO:0000781 (chromosome, telomeric region)
GO:0000785 (chromatin)
GO:0000794 (condensed nuclear chromosome)
GO:0005615 (extracellular space)
GO:0005634 (nucleus)
GO:0005654 (nucleoplasm)
GO:0005657 (replication fork)
GO:0005737 (cytoplasm)
GO:0005813 (centrosome)
GO:0005815 (microtubule organizing center)
GO:0005829 (cytosol)
GO:0005856 (cytoskeleton)
GO:0043231 (intracellular membrane-bounded organelle)
GO Molecular Function GO:0000166 (nucleotide binding)
GO:0004672 (protein kinase activity)
GO:0004674 (protein serine/threonine kinase activity)
GO:0005515 (protein binding)
GO:0005524 (ATP binding)
GO:0016301 (kinase activity)
GO:0016740 (transferase activity)
GO:0035402 (histone kinase activity (H3-T11 specific))
GO Biological Process GO:0000077 (DNA damage checkpoint)
GO:0000086 (G2/M transition of mitotic cell cycle)
GO:0006260 (DNA replication)
GO:0006281 (DNA repair)
GO:0006468 (protein phosphorylation)
GO:0006974 (cellular response to DNA damage stimulus)
GO:0006975 (DNA damage induced protein phosphorylation)
GO:0007049 (cell cycle)
GO:0010468 (regulation of gene expression)
GO:0010569 (regulation of double-strand break repair via homologous recombination)
GO:0010767 (regulation of transcription from RNA polymerase II promoter in response to UV-induced DNA damage)
GO:0016310 (phosphorylation)
GO:0018107 (peptidyl-threonine phosphorylation)
GO:0031572 (G2 DNA damage checkpoint)
GO:0035407 (histone H3-T11 phosphorylation)
GO:0042127 (regulation of cell proliferation)
GO:0045839 (negative regulation of mitotic nuclear division)
GO:0046602 (regulation of mitotic centrosome separation)
GO:0048096 (chromatin-mediated maintenance of transcription)
GO:0071260 (cellular response to mechanical stimulus)
GO:0090399 (replicative senescence)
GO:1901796 (regulation of signal transduction by p53 class mediator)
GO:2000615 (regulation of histone H3-K9 acetylation)
Wikipedia CHEK1

Target Cross References - Protein

Human Protein Atlas ENSG00000149554
IntAct O14757
Guide to Pharmacology 1987
Open Targets ENSG00000149554
PharmGKB PA110
Pharos O14757 (Tchem)
Reactome R-HSA-1433557 (Signaling by SCF-KIT.)
R-HSA-176187 (Activation of ATR in response to replication stress.)
R-HSA-5693607 (Processing of DNA double-strand break ends.)
R-HSA-5693616 (Presynaptic phase of homologous DNA pairing and strand exchange.)
R-HSA-6796648 (TP53 Regulates Transcription of DNA Repair Genes.)
R-HSA-6804756 (Regulation of TP53 Activity through Phosphorylation.)
R-HSA-69473 (G2/M DNA damage checkpoint.)
R-HSA-69601 (Ubiquitin Mediated Degradation of Phosphorylated Cdc25A.)
R-HSA-75035 (Chk1/Chk2(Cds1) mediated inactivation of Cyclin B:Cdk1 complex.)
UniProt A8K934 B4DDD0 B4DSK3 B5BTY6 F5H7S4 H2BI51 O14757

Target Cross References - Domain

InterPro IPR000719 (Prot_kinase_dom.)
IPR008271 (Ser/Thr_kinase_AS.)
IPR011009 (Kinase-like_dom.)
IPR017441 (Protein_kinase_ATP_BS.)
Pfam PF00069 (Pkinase)

Target Cross References - Structure

PDBe 1IA8 1NVQ 1NVR 1NVS 1ZLT 1ZYS 2AYP 2BR1 2BRB 2BRG 2BRH 2BRM 2BRN 2BRO 2C3J 2C3K 2C3L 2CGU 2CGV 2CGW 2CGX 2E9N 2E9O 2E9P More...
CREDO 1IA8 1NVQ 1NVR 1NVS 1ZLT 1ZYS 2AYP 2BR1 2BRB 2BRG 2BRH 2BRM 2BRN 2BRO 2C3J 2C3K 2C3L 2CGU 2CGV 2CGW 2CGX 2E9N 2E9O 2E9P More...
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