NVP-BHG712 [Ligand Id: 14226] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3752910
  • EPH receptor A1/Ephrin type-A receptor 1 in Human [ChEMBL: CHEMBL5810] [GtoPdb: 1821] [UniProtKB: P21709]
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  • EPH receptor A2/Ephrin type-A receptor 2 in Human [ChEMBL: CHEMBL2068] [GtoPdb: 1822] [UniProtKB: P29317]
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  • EPH receptor A3/Ephrin type-A receptor 3 in Human [ChEMBL: CHEMBL4954] [GtoPdb: 1823] [UniProtKB: P29320]
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  • EPH receptor A4/Ephrin type-A receptor 4 in Human [ChEMBL: CHEMBL3988] [GtoPdb: 1824] [UniProtKB: P54764]
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  • EPH receptor A5/Ephrin type-A receptor 5 in Human [ChEMBL: CHEMBL3987] [GtoPdb: 1825] [UniProtKB: P54756]
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  • EPH receptor A6/Ephrin type-A receptor 6 in Human [ChEMBL: CHEMBL4526] [GtoPdb: 1826] [UniProtKB: Q9UF33]
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  • EPH receptor A7/Ephrin type-A receptor 7 in Human [ChEMBL: CHEMBL4602] [GtoPdb: 1827] [UniProtKB: Q15375]
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  • EPH receptor A8/Ephrin type-A receptor 8 in Human [ChEMBL: CHEMBL4134] [GtoPdb: 1828] [UniProtKB: P29322]
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  • EPH receptor B2/Ephrin type-B receptor 2 in Human [ChEMBL: CHEMBL3290] [GtoPdb: 1831] [UniProtKB: P29323]
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  • EPH receptor B3/Ephrin type-B receptor 3 in Human [ChEMBL: CHEMBL4901] [GtoPdb: 1832] [UniProtKB: P54753]
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  • EPH receptor B4/Ephrin type-B receptor 4 in Human [ChEMBL: CHEMBL5147] [GtoPdb: 1833] [UniProtKB: P54760]
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  • EPH receptor B6/Ephrin type-B receptor 6 in Human [ChEMBL: CHEMBL5836] [GtoPdb: 1834] [UniProtKB: O15197]
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  • Raf-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase RAF in Human [ChEMBL: CHEMBL1906] [GtoPdb: 2184] [UniProtKB: P04049]
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  • ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
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  • SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
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  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
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  • TBC1 domain family member 15 in Human [GtoPdb: 3328] [UniProtKB: Q8TC07]
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  • SAM and HD domain containing deoxynucleoside triphosphate triphosphohydrolase 1 in Human [GtoPdb: 3330] [UniProtKB: Q9Y3Z3]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
EPH receptor A1/Ephrin type-A receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5810] [GtoPdb: 1821] [UniProtKB: P21709]
ChEMBL Selectivity interaction (NanoBRET assay (HEK293T cells)) EUB0000143b EPHA1 B 6.52 pIC50 303.4 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
EPH receptor A2/Ephrin type-A receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2068] [GtoPdb: 1822] [UniProtKB: P29317]
GtoPdb - - 7.89 pKd 13 nM Kd ChemMedChem (2018) 13: 1629-1633 [PMID:29928781]
ChEMBL Affinity Biochemical interaction (Microscale thermophoresis (MST) assay) EUB0000143b EPHA2 B 7.89 pIC50 13 nM IC50 Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Selectivity interaction (NanoBRET assay (HEK293T cells)) EUB0000143b EPHA2 B 8.48 pIC50 3.3 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Affinity On-target Cellular interaction (NanoBRET assay (HEK293T cells)) EUB0000143b EPHA2 B 8.52 pIC50 3 nM IC50 Affinity On-target Cellular Literature for EUbOPEN Chemogenomics Library wave 3
EPH receptor A3/Ephrin type-A receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4954] [GtoPdb: 1823] [UniProtKB: P29320]
ChEMBL Selectivity interaction (NanoBRET assay (HEK293T cells)) EUB0000143b EPHA3 B 9.52 pIC50 0.3 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
EPH receptor A4/Ephrin type-A receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3988] [GtoPdb: 1824] [UniProtKB: P54764]
ChEMBL Selectivity interaction (NanoBRET assay (HEK293T cells)) EUB0000143b EPHA4 B 8.12 pIC50 7.6 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
EPH receptor A5/Ephrin type-A receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3987] [GtoPdb: 1825] [UniProtKB: P54756]
ChEMBL Selectivity interaction (NanoBRET assay (HEK293T cells)) EUB0000143b EPHA5 B 8.55 pIC50 2.8 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
EPH receptor A6/Ephrin type-A receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4526] [GtoPdb: 1826] [UniProtKB: Q9UF33]
ChEMBL Selectivity interaction (NanoBRET assay (HEK293T cells)) EUB0000143b EPHA6 B 6.58 pIC50 263 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
EPH receptor A7/Ephrin type-A receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4602] [GtoPdb: 1827] [UniProtKB: Q15375]
ChEMBL Selectivity interaction (NanoBRET assay (HEK293T cells)) EUB0000143b EPHA7 B 4.3 pIC50 >50000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
EPH receptor A8/Ephrin type-A receptor 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4134] [GtoPdb: 1828] [UniProtKB: P29322]
ChEMBL Selectivity interaction (NanoBRET assay (HEK293T cells)) EUB0000143b EPHA8 B 8.92 pIC50 1.2 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
EPH receptor B2/Ephrin type-B receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3290] [GtoPdb: 1831] [UniProtKB: P29323]
ChEMBL Selectivity interaction (NanoBRET assay (HEK293T cells)) EUB0000143b EPHB2 B 8.6 pIC50 2.5 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
EPH receptor B3/Ephrin type-B receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4901] [GtoPdb: 1832] [UniProtKB: P54753]
ChEMBL Selectivity interaction (NanoBRET assay (HEK293T cells)) EUB0000143b EPHB3 B 8.22 pIC50 6 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
EPH receptor B4/Ephrin type-B receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5147] [GtoPdb: 1833] [UniProtKB: P54760]
GtoPdb - - 8.22 pKd 6 nM Kd ChemMedChem (2018) 13: 1629-1633 [PMID:29928781]
ChEMBL Affinity Biochemical interaction (Microscale thermophoresis (MST) assay) EUB0000143b EPHB4 B 8.22 pIC50 6 nM IC50 Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Affinity On-target Cellular interaction (NanoBRET assay (HEK293T cells)) EUB0000143b EPHB4 B 8.52 pIC50 3 nM IC50 Affinity On-target Cellular Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Selectivity interaction (NanoBRET assay (HEK293T cells)) EUB0000143b EPHB4 B 8.52 pIC50 3 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
EPH receptor B6/Ephrin type-B receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5836] [GtoPdb: 1834] [UniProtKB: O15197]
ChEMBL Selectivity interaction (NanoBRET assay (HEK293T cells)) EUB0000143b EPHB6 B 5.35 pIC50 4477.1 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
Raf-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase RAF in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1906] [GtoPdb: 2184] [UniProtKB: P04049]
ChEMBL Selectivity interaction (Kinase panel (TR-FRET-based LanthaScreen™ and Caliper mobility shift assays)) EUB0000143b RAF1 B 6.4 pIC50 395 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
ChEMBL Selectivity interaction (Kinase panel (TR-FRET-based LanthaScreen™ and Caliper mobility shift assays)) EUB0000143b ABL1 B 5.78 pIC50 1667 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
ChEMBL Selectivity interaction (Kinase panel (TR-FRET-based LanthaScreen™ and Caliper mobility shift assays)) EUB0000143b SRC B 5.9 pIC50 1266 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
ChEMBL Inhibition of VEGFR2 (unknown origin) autophosphorylation after 2 hrs by cell-based assay B 5.38 pEC50 4200 nM EC50 Medchemcomm (2015) 6: 1518-1534
TBC1 domain family member 15 in Human [GtoPdb: 3328] [UniProtKB: Q8TC07]
GtoPdb Binding affinity determined in a Kinobeads assay - 6.2 pKd 624 nM Kd ChemMedChem (2018) 13: 1629-1633 [PMID:29928781]
SAM and HD domain containing deoxynucleoside triphosphate triphosphohydrolase 1 in Human [GtoPdb: 3330] [UniProtKB: Q9Y3Z3]
GtoPdb - - 8.44 pKd 3.6 nM Kd ChemMedChem (2018) 13: 1629-1633 [PMID:29928781]

ChEMBL data shown on this page come from version 35:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]