Target family: CHK1 subfamily (type: enzyme)
Target: checkpoint kinase 1

Ligand: 7-hydroxystaurosporine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity:  pIC50
Reference (Journal): p53-deficient cells rely on ATM- and ATR-mediated checkpoint signaling through the p38MAPK/MK2 pathway for survival after DNA damage.
Published in: Cancer Cell

Ligand: 7-hydroxystaurosporine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Inhibition of Chk1 by the G2 DNA damage checkpoint inhibitor isogranulatimide.
Published in: Mol Cancer Ther

Ligand: 7-hydroxystaurosporine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity:  pIC50
Reference (Journal): The radiosensitizing agent 7-hydroxystaurosporine (UCN-01) inhibits the DNA damage checkpoint kinase hChk1.
Published in: Cancer Res

Ligand: AZD7762 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Discovery of checkpoint kinase inhibitor (S)-5-(3-fluorophenyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide (AZD7762) by structure-based design and optimization of thiophenecarboxamide ureas.
Published in: J Med Chem

Ligand: BX-795 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.289999961853027 pIC50
Reference (Journal): Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1.
Published in: J Biol Chem

Ligand: BX-912 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.079999923706055 pIC50
Reference (Journal): Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1.
Published in: J Biol Chem

Ligand: CCT241533 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.71999979019165 pIC50
Reference (Journal): CCT241533 is a potent and selective inhibitor of CHK2 that potentiates the cytotoxicity of PARP inhibitors.
Published in: Cancer Res

Ligand: CCT244747 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.109999656677246 pIC50
Reference (Journal): Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors.
Published in: J Med Chem

Ligand: CCT245737 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.890000343322754 pIC50
Reference (Journal): Multiparameter Lead Optimization to Give an Oral Checkpoint Kinase 1 (CHK1) Inhibitor Clinical Candidate: (R)-5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737).
Published in: J Med Chem

Ligand: CHIR-124 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.489999771118164 pIC50
Reference (Journal): 4-(Aminoalkylamino)-3-benzimidazole-quinolinones as potent CHK-1 inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: compound 25 [PMID: 17935989] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.
Published in: Bioorg Med Chem Lett

Ligand: compound 25 [PMID: 20855207] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.849999904632568 pIC50
Reference (Journal): Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: compound 33 [PMID: 19364658] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.050000190734863 pIC50
Reference (Journal): Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).
Published in: Bioorg Med Chem

Ligand: isogranulatimide (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7 pIC50
Reference (Journal): Inhibition of Chk1 by the G2 DNA damage checkpoint inhibitor isogranulatimide.
Published in: Mol Cancer Ther

Ligand: isogranulatimide (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7 pIC50
Reference (Journal): Synthesis, checkpoint kinase 1 inhibitory properties and in vitro antiproliferative activities of new pyrrolocarbazoles.
Published in: Bioorg Med Chem

Ligand: MK-8776 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.520000457763672 pIC50
Reference (Journal): Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: a template-based approach--part 2.
Published in: Bioorg Med Chem Lett

Ligand: PF-477736 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.3100004196167 pIC50
Reference (Journal): Breaching the DNA damage checkpoint via PF-00477736, a novel small-molecule inhibitor of checkpoint kinase 1.
Published in: Mol Cancer Ther

Ligand: prexasertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.050000190734863 pIC50
Reference (Journal): LY2606368 Causes Replication Catastrophe and Antitumor Effects through CHK1-Dependent Mechanisms.
Published in: Mol Cancer Ther

Ligand: rabusertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.149999618530273 pIC50
Reference (Journal): Characterization and preclinical development of LY2603618: a selective and potent Chk1 inhibitor.
Published in: Invest New Drugs

Ligand: SB 218078 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.820000171661377 pIC50
Reference (Journal): An indolocarbazole inhibitor of human checkpoint kinase (Chk1) abrogates cell cycle arrest caused by DNA damage.
Published in: Cancer Res