dwb2023/gtopdb-target-family-interaction-detail huggingface dataset:
Target family: Type II RTKs: Insulin receptor family (type: catalytic_receptor)
Target: Insulin receptor

Ligand: BMS-536924 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.139999866485596 pIC50
Reference (Journal): Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity.
Published in: J Med Chem
Target family: Type I PIP kinases (1-phosphatidylinositol-4-phosphate 5-kinase family) (type: enzyme)
Target: phosphatidylinositol-4-phosphate 5-kinase type 1 alpha

Ligand: ISA-2011B (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity:  -
Reference (Journal): The role of PI3K/AKT-related PIP5K1α and the discovery of its selective inhibitor for treatment of advanced prostate cancer.
Published in: Proc Natl Acad Sci USA
Target family: Type I receptor serine/threonine kinases (type: catalytic_receptor)
Target: activin A receptor type 1B

Ligand: BMS-986260 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.480000019073486 pIC50
Reference (Journal): Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGFβR1 Inhibitor as an Immuno-oncology Agent.
Published in: ACS Med Chem Lett

Ligand: compound 13d [PMID: 23639540] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.489999771118164 pIC50
Reference (Journal): Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe.
Published in: Bioorg Med Chem Lett

Ligand: compound 13r [PMID: 23639540] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.739999771118164 pIC50
Reference (Journal): Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe.
Published in: Bioorg Med Chem Lett

Ligand: galunisertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.110000133514404 pIC50
Reference (Journal): Preclinical assessment of galunisertib (LY2157299 monohydrate), a first-in-class transforming growth factor-β receptor type I inhibitor.
Published in: Oncotarget

Ligand: vactosertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.889999866485596 pIC50
Reference (Journal): Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/antifibrotic agent.
Published in: J Med Chem
Target family: Type I receptor serine/threonine kinases (type: catalytic_receptor)
Target: activin A receptor type 1C

Ligand: SB-431542 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Synthesis and biological evaluation of 1,2,4-trisubstituted imidazoles and 1,3,5-trisubstituted pyrazoles as inhibitors of transforming growth factor beta type 1 receptor (ALK5).
Published in: Bioorg Med Chem Lett

Ligand: SB-431542 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Synthesis and SAR of b-annulated 1,4-dihydropyridines define cardiomyogenic compounds as novel inhibitors of TGFβ signaling.
Published in: J Med Chem
Target family: Type I receptor serine/threonine kinases (type: catalytic_receptor)
Target: activin A receptor type IL

Ligand: compound 13a [PMID: 23639540] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.380000114440918 pIC50
Reference (Journal): Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe.
Published in: Bioorg Med Chem Lett

Ligand: compound 13d [PMID: 23639540] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe.
Published in: Bioorg Med Chem Lett

Ligand: compound 13r [PMID: 23639540] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe.
Published in: Bioorg Med Chem Lett

Ligand: LDN-214117 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.570000171661377 pIC50
Reference (Journal): Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants.
Published in: J Med Chem

Ligand: ML347 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.340000152587891 pIC50
Reference (Journal): Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe.
Published in: Bioorg Med Chem Lett

Ligand: panulisib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.329999923706055 pIC50
Reference (Journal): P7170: A Novel Molecule with Unique Profile of mTORC1/C2 and Activin Receptor-like Kinase 1 Inhibition Leading to Antitumor and Antiangiogenic Activity.
Published in: Mol Cancer Ther

Ligand: zilurgisertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.489999771118164 pIC50
Reference (Patent): Aminopyridine derivatives and their use as selective alk-2 inhibitors
Target family: Type I receptor serine/threonine kinases (type: catalytic_receptor)
Target: bone morphogenetic protein receptor type IA

Ligand: compound 13a [PMID: 23639540] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.980000019073486 pIC50
Reference (Journal): Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe.
Published in: Bioorg Med Chem Lett

Ligand: compound 13d [PMID: 23639540] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe.
Published in: Bioorg Med Chem Lett

Ligand: compound 13r [PMID: 23639540] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe.
Published in: Bioorg Med Chem Lett

Ligand: K02288 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.460000038146973 pIC50
Reference (Journal): Inhibition of ALK2 with bicyclic pyridyllactams.
Published in: Bioorg Med Chem Lett

Ligand: LDN-214117 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.929999828338623 pIC50
Reference (Journal): Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants.
Published in: J Med Chem

Ligand: ML347 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 4.96999979019165 pIC50
Reference (Journal): Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe.
Published in: Bioorg Med Chem Lett

Ligand: zilurgisertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.039999961853027 pIC50
Reference (Patent): Aminopyridine derivatives and their use as selective alk-2 inhibitors
Target family: Type I receptor serine/threonine kinases (type: catalytic_receptor)
Target: bone morphogenetic protein receptor type IB

Ligand: compound 13a [PMID: 23639540] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.21999979019165 pIC50
Reference (Journal): Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe.
Published in: Bioorg Med Chem Lett

Ligand: compound 13d [PMID: 23639540] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe.
Published in: Bioorg Med Chem Lett

Ligand: compound 13r [PMID: 23639540] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe.
Published in: Bioorg Med Chem Lett

Ligand: galunisertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.329999923706055 pIC50
Reference (Journal): Preclinical assessment of galunisertib (LY2157299 monohydrate), a first-in-class transforming growth factor-β receptor type I inhibitor.
Published in: Oncotarget

Ligand: zilurgisertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.480000019073486 pIC50
Reference (Patent): Aminopyridine derivatives and their use as selective alk-2 inhibitors
Target family: Type I receptor serine/threonine kinases (type: catalytic_receptor)
Target: transforming growth factor beta receptor 1

Ligand: BIX02189 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.239999771118164 pIC50
Reference (Journal): Identification of pharmacological inhibitors of the MEK5/ERK5 pathway.
Published in: Biochem Biophys Res Commun

Ligand: BMS-986260 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.800000190734863 pIC50
Reference (Journal): Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGFβR1 Inhibitor as an Immuno-oncology Agent.
Published in: ACS Med Chem Lett

Ligand: compound 13d [PMID: 23639540] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.75 pIC50
Reference (Journal): Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe.
Published in: Bioorg Med Chem Lett

Ligand: compound 13r [PMID: 23639540] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.119999885559082 pIC50
Reference (Journal): Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe.
Published in: Bioorg Med Chem Lett
Target family: Type I RTKs: ErbB (epidermal growth factor) receptor family (type: catalytic_receptor)
Target: erb-b2 receptor tyrosine kinase 3

Ligand: elgemtumab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity:  pKd
Reference (Patent): Antibodies for epidermal growth factor receptor 3 (HER3).

Ligand: istiratumab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity: 9 pKd
Reference (Journal): MM-141, an IGF-IR- and ErbB3-directed bispecific antibody, overcomes network adaptations that limit activity of IGF-IR inhibitors.
Published in: Mol Cancer Ther

Ligand: MM-111 (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity: 7.809999942779541 pKd
Reference (Journal): Antitumor activity of a novel bispecific antibody that targets the ErbB2/ErbB3 oncogenic unit and inhibits heregulin-induced activation of ErbB3.
Published in: Mol Cancer Ther

Ligand: neuregulin-1 (Peptide)
Interaction type: None
Action: None
Ligand approved: no
Median affinity:  -

Ligand: neuregulin-2 (Peptide)
Interaction type: None
Action: None
Ligand approved: no
Median affinity:  -

Ligand: sapitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Discovery of AZD8931, an Equipotent, Reversible Inhibitor of Signaling by EGFR, HER2, and HER3 Receptors.
Published in: ACS Med Chem Lett

Ligand: seribantumab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity: 9.109999656677246 pKd
Reference (Journal): Therapeutically targeting ErbB3: a key node in ligand-induced activation of the ErbB receptor-PI3K axis.
Published in: Sci Signal

Ligand: TX1-85-1 (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity: 7.639999866485596 pIC50
Reference (Journal): Development of small molecules targeting the pseudokinase Her3.
Published in: Bioorg Med Chem Lett

Ligand: TX2-121-1 (Synthetic organic)
Interaction type: Inhibitor
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity: 7.309999942779541 pIC50
Reference (Journal): Development of small molecules targeting the pseudokinase Her3.
Published in: Bioorg Med Chem Lett
Target family: Type IV RTKs: VEGF (vascular endothelial growth factor) receptor family (type: catalytic_receptor)
Target: fms related receptor tyrosine kinase 4

Ligand: compound 38k [PMID: 34351741] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.960000038146973 pIC50
Reference (Journal): Discovery, Synthesis, and Evaluation of Highly Selective Vascular Endothelial Growth Factor Receptor 3 (VEGFR3) Inhibitor for the Potential Treatment of Metastatic Triple-Negative Breast Cancer.
Published in: J Med Chem
Target family: Type IX RTKs: MuSK (type: catalytic_receptor)
Target: muscle associated receptor tyrosine kinase

Ligand: compound 1d [PMID: 21493067] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.650000095367432 pIC50
Reference (Journal): In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: compound 25 [PMID: 17935989] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.78000020980835 pKi
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
Target family: Type VII RTKs: Neurotrophin receptor/Trk family (type: catalytic_receptor)
Target: neurotrophic receptor tyrosine kinase 1

Ligand: anizatrectinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.960000038146973 pIC50
Reference (Patent): 1-((3s,4r)-4-(3-fluorophenyl)-1-(2-methoxyethyl)pyrrolidin-3-yl)-3-(4-methyl-3-(2-methylpyrimidin-5-yl)-1-phenyl-1h-pyrazol-5-yl)urea as a trka kinase inhibitor
Target family: Type V RTKs: FGF (fibroblast growth factor) receptor family (type: catalytic_receptor)
Target: fibroblast growth factor receptor 1

Ligand: brivanib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pKd
Reference (Journal): Comprehensive analysis of kinase inhibitor selectivity.
Published in: Nat Biotechnol
Target family: Type V RTKs: FGF (fibroblast growth factor) receptor family (type: catalytic_receptor)
Target: fibroblast growth factor receptor 3

Ligand: compound 29 [PMID: 36356320] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.569999694824219 pIC50
Reference (Journal): Discovery of Potent and Selective Inhibitors of Wild-Type and Gatekeeper Mutant Fibroblast Growth Factor Receptor (FGFR) 2/3.
Published in: J Med Chem

Ligand: compound 1d [PMID: 21493067] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.940000057220459 pIC50
Reference (Journal): In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: BLU-9931 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.820000171661377 pIC50
Reference (Journal): First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway.
Published in: Cancer Discov

Ligand: ASP5878 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.680000305175781 pIC50
Reference (Journal): Discovery of ASP5878: Synthesis and structure-activity relationships of pyrimidine derivatives as pan-FGFRs inhibitors with improved metabolic stability and suppressed hERG channel inhibitory activity.
Published in: Bioorg Med Chem
Target family: Type XIII RTKs: Ephrin receptor family (type: catalytic_receptor)
Target: EPH receptor B2

Ligand: DDR1/2 inhibitor 5n (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.590000152587891 pKd
Reference (Journal): Design, Synthesis, and Biological Evaluation of 3-(Imidazo[1,2- a]pyrazin-3-ylethynyl)-4-isopropyl- N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)benzamide as a Dual Inhibitor of Discoidin Domain Receptors 1 and 2.
Published in: J Med Chem
Target family: Type XIII RTKs: Ephrin receptor family (type: catalytic_receptor)
Target: EPH receptor A7

Ligand: compound 66 [PMID: 19788238] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.949999809265137 pIC50
Reference (Journal): Structure-based optimization of potent and selective inhibitors of the tyrosine kinase erythropoietin producing human hepatocellular carcinoma receptor B4 (EphB4).
Published in: J Med Chem

Ligand: compound 8h [PMID: 21561767] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.380000114440918 pIC50
Reference (Journal): Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.
Published in: Bioorg Med Chem Lett

Ligand: DDR1/2 inhibitor 5n (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.699999809265137 pKd
Reference (Journal): Design, Synthesis, and Biological Evaluation of 3-(Imidazo[1,2- a]pyrazin-3-ylethynyl)-4-isopropyl- N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)benzamide as a Dual Inhibitor of Discoidin Domain Receptors 1 and 2.
Published in: J Med Chem
Target family: Type XIII RTKs: Ephrin receptor family (type: catalytic_receptor)
Target: EPH receptor A8

Ligand: compound 20 [PMID: 23489211] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.820000171661377 pIC50
Reference (Journal): Amino acid conjugates of lithocholic acid as antagonists of the EphA2 receptor.
Published in: J Med Chem

Ligand: compound 66 [PMID: 19788238] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.350000381469727 pIC50
Reference (Journal): Structure-based optimization of potent and selective inhibitors of the tyrosine kinase erythropoietin producing human hepatocellular carcinoma receptor B4 (EphB4).
Published in: J Med Chem

Ligand: DDR1/2 inhibitor 5n (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.099999904632568 pKd
Reference (Journal): Design, Synthesis, and Biological Evaluation of 3-(Imidazo[1,2- a]pyrazin-3-ylethynyl)-4-isopropyl- N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)benzamide as a Dual Inhibitor of Discoidin Domain Receptors 1 and 2.
Published in: J Med Chem

Ligand: RIPK3 inhibitor 18 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.590000152587891 pIC50
Reference (Journal): Identification of RIPK3 Type II Inhibitors Using High-Throughput Mechanistic Studies in Hit Triage
Published in: ACS Med Chem Lett