dorsomorphin [Ligand Id: 4907] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL478629 (Dorsomorphin)
  • activin A receptor type 1/Activin receptor type-1 in Human [ChEMBL: CHEMBL5903] [GtoPdb: 1785] [UniProtKB: Q04771]
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  • activin A receptor type 1B/Activin receptor type-1B in Human [ChEMBL: CHEMBL5310] [GtoPdb: 1787] [UniProtKB: P36896]
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  • protein kinase AMP-activated non-catalytic subunit beta 2/protein kinase AMP-activated non-catalytic subunit gamma 1/protein kinase AMP-activated catalytic subunit alpha 2/protein kinase AMP-activated catalytic subunit alpha 1/protein kinase AMP-activated non-catalytic subunit gamma 3/protein kinase AMP-activated non-catalytic subunit gamma 2/protein kinase AMP-activated non-catalytic subunit beta 1/AMP-activated protein kinase, AMPK in Human [ChEMBL: CHEMBL2096907] [GtoPdb: 1544154515421541154715461543] [UniProtKB: O43741P54619P54646Q13131Q9UGI9Q9UGJ0Q9Y478]
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  • protein kinase AMP-activated non-catalytic subunit beta 1/AMP-activated protein kinase, beta-1 subunit in Human [ChEMBL: CHEMBL3847] [GtoPdb: 1543] [UniProtKB: Q9Y478]
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  • Bone morphogenetic protein 4 in Human [ChEMBL: CHEMBL5350] [UniProtKB: P12644]
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  • bone morphogenetic protein receptor type IA/Bone morphogenetic protein receptor type-1A in Human [ChEMBL: CHEMBL5275] [GtoPdb: 1786] [UniProtKB: P36894]
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  • bone morphogenetic protein receptor type IB/Bone morphogenetic protein receptor type-1B in Human [ChEMBL: CHEMBL5476] [GtoPdb: 1789] [UniProtKB: O00238]
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  • bone morphogenetic protein receptor type 2/Bone morphogenetic protein receptor type-2 in Human [ChEMBL: CHEMBL5467] [GtoPdb: 1794] [UniProtKB: Q13873]
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  • EPH receptor A2/Ephrin type-A receptor 2 in Human [ChEMBL: CHEMBL2068] [GtoPdb: 1822] [UniProtKB: P29317]
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  • eukaryotic translation initiation factor 2 alpha kinase 2/Interferon-induced, double-stranded RNA-activated protein kinase in Human [ChEMBL: CHEMBL5785] [GtoPdb: 2016] [UniProtKB: P19525]
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  • MAPK interacting serine/threonine kinase 1/MAP kinase-interacting serine/threonine-protein kinase MNK1 in Human [ChEMBL: CHEMBL4718] [GtoPdb: 2104] [UniProtKB: Q9BUB5]
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  • ribosomal protein S6 kinase A1/Ribosomal protein S6 kinase alpha 1 in Human [ChEMBL: CHEMBL2553] [GtoPdb: 1527] [UniProtKB: Q15418]
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  • activin A receptor type IL/Serine/threonine-protein kinase receptor R3 in Human [ChEMBL: CHEMBL5311] [GtoPdb: 1784] [UniProtKB: P37023]
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  • transforming growth factor beta receptor 1/TGF-beta receptor type I in Human [ChEMBL: CHEMBL4439] [GtoPdb: 1788] [UniProtKB: P36897]
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  • transforming growth factor beta receptor 2/TGF-beta receptor type II in Human [ChEMBL: CHEMBL4267] [GtoPdb: 1795] [UniProtKB: P37173]
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  • LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
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  • fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
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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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  • YES proto-oncogene 1, Src family tyrosine kinase/Tyrosine-protein kinase YES in Human [ChEMBL: CHEMBL2073] [GtoPdb: 2284] [UniProtKB: P07947]
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  • fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948]
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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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  • AMP kinase in Human [GtoPdb: 1540]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
activin A receptor type 1/Activin receptor type-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5903] [GtoPdb: 1785] [UniProtKB: Q04771]
ChEMBL Kinase Assay: Kinase assays were performed using the assay kit by Reaction Biology Corp (Malvern, Pa.). The compounds were tested at 10 concentrations by 3-fold serial dilutions starting at 30 μM. Staurosporin was used as a control nonspecific kinase inhibitor. In vitro kinase reactions using purified kinases were carried out in the presence of 10 μM ATP and test compounds. B 6.83 pIC50 148.1 nM IC50 US-9040694-B1. Compounds and methods useful for directing stem cell differentiation (2015)
ChEMBL Inhibition of ALK2 (unknown origin) B 7.17 pIC50 67.5 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 3248-3252 [PMID:23639540]
activin A receptor type 1B/Activin receptor type-1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5310] [GtoPdb: 1787] [UniProtKB: P36896]
ChEMBL Inhibition of ALK4 (unknown origin) B 4.59 pIC50 25740 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 3248-3252 [PMID:23639540]
protein kinase AMP-activated non-catalytic subunit beta 2/protein kinase AMP-activated non-catalytic subunit gamma 1/protein kinase AMP-activated catalytic subunit alpha 2/protein kinase AMP-activated catalytic subunit alpha 1/protein kinase AMP-activated non-catalytic subunit gamma 3/protein kinase AMP-activated non-catalytic subunit gamma 2/protein kinase AMP-activated non-catalytic subunit beta 1/AMP-activated protein kinase, AMPK in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2096907] [GtoPdb: 1544154515421541154715461543] [UniProtKB: O43741P54619P54646Q13131Q9UGI9Q9UGJ0Q9Y478]
ChEMBL Inhibition of human AMPK in presence of (33P)gamma ATP B 6.64 pIC50 230 nM IC50 J. Med. Chem. (2015) 58: 9451-9479 [PMID:26288266]
ChEMBL Inhibition of human AMPK alpha-2/beta-1/gamma-1 by Hot Spot filtration binding assay B 7.39 pIC50 41 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 6394-6399 [PMID:20932747]
protein kinase AMP-activated non-catalytic subunit beta 1/AMP-activated protein kinase, beta-1 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3847] [GtoPdb: 1543] [UniProtKB: Q9Y478]
ChEMBL Kinase Assay: Kinase assays were performed using the assay kit by Reaction Biology Corp (Malvern, Pa.). The compounds were tested at 10 concentrations by 3-fold serial dilutions starting at 30 μM. Staurosporin was used as a control nonspecific kinase inhibitor. In vitro kinase reactions using purified kinases were carried out in the presence of 10 μM ATP and test compounds. B 6.5 pIC50 318.2 nM IC50 US-9040694-B1. Compounds and methods useful for directing stem cell differentiation (2015)
ChEMBL Inhibition of AMPK (unknown origin) B 6.63 pIC50 234.6 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 3248-3252 [PMID:23639540]
Bone morphogenetic protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5350] [UniProtKB: P12644]
ChEMBL Inhibition of BMP4-induced phosphorylation of SMAD 1/5/8 by cytoblot cellular ELISA B 6.37 pIC50 430 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 4388-4392 [PMID:18621530]
bone morphogenetic protein receptor type IA/Bone morphogenetic protein receptor type-1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5275] [GtoPdb: 1786] [UniProtKB: P36894]
ChEMBL Inhibition of ALK3 (unknown origin) B 7.02 pIC50 95 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 3248-3252 [PMID:23639540]
bone morphogenetic protein receptor type IB/Bone morphogenetic protein receptor type-1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5476] [GtoPdb: 1789] [UniProtKB: O00238]
ChEMBL Inhibition of ALK6 (unknown origin) by radioisotopic assay B 6.33 pIC50 467 nM IC50 J. Med. Chem. (2014) 57: 4213-4238 [PMID:24786585]
ChEMBL Inhibition of ALK6 (unknown origin) B 6.63 pIC50 235 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 3248-3252 [PMID:23639540]
bone morphogenetic protein receptor type 2/Bone morphogenetic protein receptor type-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5467] [GtoPdb: 1794] [UniProtKB: Q13873]
ChEMBL Inhibition of BMPR2 (unknown origin) B 7.13 pIC50 74 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 3248-3252 [PMID:23639540]
EPH receptor A2/Ephrin type-A receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2068] [GtoPdb: 1822] [UniProtKB: P29317]
ChEMBL Inhibition of EphA2 by Hot Spot filtration binding assay B 7.96 pIC50 11 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 6394-6399 [PMID:20932747]
GtoPdb Assayed using AMPK heterotrimeric complex containing α2, β1, γ1 subunits - 7.96 pIC50 11 nM IC50 Bioorg Med Chem Lett (2010) 20: 6394-9 [PMID:20932747]
eukaryotic translation initiation factor 2 alpha kinase 2/Interferon-induced, double-stranded RNA-activated protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5785] [GtoPdb: 2016] [UniProtKB: P19525]
ChEMBL Inhibition of human recombinant PKR autophosphorylation using poly[I:C] after 10 mins by luminescent assay B 4.8 pIC50 16000 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 4108-4114 [PMID:21632247]
MAPK interacting serine/threonine kinase 1/MAP kinase-interacting serine/threonine-protein kinase MNK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4718] [GtoPdb: 2104] [UniProtKB: Q9BUB5]
ChEMBL Inhibition of MNK1 by Hot Spot filtration binding assay B 7.96 pIC50 11 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 6394-6399 [PMID:20932747]
GtoPdb Assayed using AMPK heterotrimeric complex containing α2, β1, γ1 subunits - 7.96 pIC50 11 nM IC50 Bioorg Med Chem Lett (2010) 20: 6394-9 [PMID:20932747]
ribosomal protein S6 kinase A1/Ribosomal protein S6 kinase alpha 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2553] [GtoPdb: 1527] [UniProtKB: Q15418]
ChEMBL Inhibition of RSK1 by Hot Spot filtration binding assay B 6.68 pIC50 210 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 6394-6399 [PMID:20932747]
GtoPdb Assayed using AMPK heterotrimeric complex containing α2, β1, γ1 subunits - 6.68 pIC50 210 nM IC50 Bioorg Med Chem Lett (2010) 20: 6394-9 [PMID:20932747]
activin A receptor type IL/Serine/threonine-protein kinase receptor R3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5311] [GtoPdb: 1784] [UniProtKB: P37023]
ChEMBL Inhibition of ALK1 (unknown origin) B 6.97 pIC50 106.3 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 3248-3252 [PMID:23639540]
transforming growth factor beta receptor 1/TGF-beta receptor type I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4439] [GtoPdb: 1788] [UniProtKB: P36897]
ChEMBL Inhibition of ALK5 (unknown origin) B 4.77 pIC50 17090 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 3248-3252 [PMID:23639540]
ChEMBL Kinase Assay: Kinase assays were performed using the assay kit by Reaction Biology Corp (Malvern, Pa.). The compounds were tested at 10 concentrations by 3-fold serial dilutions starting at 30 μM. Staurosporin was used as a control nonspecific kinase inhibitor. In vitro kinase reactions using purified kinases were carried out in the presence of 10 μM ATP and test compounds. B 4.97 pIC50 10760 nM IC50 US-9040694-B1. Compounds and methods useful for directing stem cell differentiation (2015)
ChEMBL Inhibition of human ALK5 in presence of (33P)gamma ATP B 5 pIC50 10000 nM IC50 J. Med. Chem. (2015) 58: 9451-9479 [PMID:26288266]
transforming growth factor beta receptor 2/TGF-beta receptor type II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4267] [GtoPdb: 1795] [UniProtKB: P37173]
ChEMBL Inhibition of TGFBR2 (unknown origin) B 6.99 pIC50 102.9 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 3248-3252 [PMID:23639540]
LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
ChEMBL Inhibition of LCK by Hot Spot filtration binding assay B 7.8 pIC50 16 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 6394-6399 [PMID:20932747]
GtoPdb Assayed using AMPK heterotrimeric complex containing α2, β1, γ1 subunits - 7.8 pIC50 16 nM IC50 Bioorg Med Chem Lett (2010) 20: 6394-9 [PMID:20932747]
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
GtoPdb Assayed using AMPK heterotrimeric complex containing α2, β1, γ1 subunits - 9 pIC50 <1 nM IC50 Bioorg Med Chem Lett (2010) 20: 6394-9 [PMID:20932747]
ChEMBL Inhibition of FLT3 by Hot Spot filtration binding assay B 9 pIC50 <1 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 6394-6399 [PMID:20932747]
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
ChEMBL Inhibition of c-SRC by Hot Spot filtration binding assay B 8.7 pIC50 2 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 6394-6399 [PMID:20932747]
GtoPdb Assayed using AMPK heterotrimeric complex containing α2, β1, γ1 subunits - 8.7 pIC50 2 nM IC50 Bioorg Med Chem Lett (2010) 20: 6394-9 [PMID:20932747]
YES proto-oncogene 1, Src family tyrosine kinase/Tyrosine-protein kinase YES in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073] [GtoPdb: 2284] [UniProtKB: P07947]
ChEMBL Inhibition of Yes1 (unknown origin) assessed as kinase-dependent enzymatic production of ADP from ATP using coupled luminescence-based reaction by ADP-Glo kinase assay B 6.71 pIC50 195.9 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 4398-4403 [PMID:23787099]
ChEMBL Inhibition of Yes1 (unknown origin) by [gamma-33P]-ATP radiolabeled enzyme activity assay B 7.53 pIC50 29.8 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 4398-4403 [PMID:23787099]
fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948]
ChEMBL Inhibition of FLT1 by Hot Spot filtration binding assay B 7.96 pIC50 11 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 6394-6399 [PMID:20932747]
GtoPdb Assayed using AMPK heterotrimeric complex containing α2, β1, γ1 subunits - 7.96 pIC50 11 nM IC50 Bioorg Med Chem Lett (2010) 20: 6394-9 [PMID:20932747]
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 human KDR in presence of (33P)gamma ATP B 6.66 pIC50 220 nM IC50 J. Med. Chem. (2015) 58: 9451-9479 [PMID:26288266]
ChEMBL Kinase Assay: Kinase assays were performed using the assay kit by Reaction Biology Corp (Malvern, Pa.). The compounds were tested at 10 concentrations by 3-fold serial dilutions starting at 30 μM. Staurosporin was used as a control nonspecific kinase inhibitor. In vitro kinase reactions using purified kinases were carried out in the presence of 10 μM ATP and test compounds. B 7.6 pIC50 25.14 nM IC50 US-9040694-B1. Compounds and methods useful for directing stem cell differentiation (2015)
ChEMBL Inhibition of KDR (unknown origin) B 7.66 pIC50 21.8 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 3248-3252 [PMID:23639540]
ChEMBL Inhibition of KDR by Hot Spot filtration binding assay B 8.4 pIC50 4 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 6394-6399 [PMID:20932747]
GtoPdb Assayed using AMPK heterotrimeric complex containing α2, β1, γ1 subunits - 8.4 pIC50 4 nM IC50 Bioorg Med Chem Lett (2010) 20: 6394-9 [PMID:20932747]
AMP kinase in Human [GtoPdb: 1540]
GtoPdb Assayed using AMPK heterotrimeric complex containing α2, β1, γ1 subunits - 7.39 pIC50 41 nM IC50 Bioorg Med Chem Lett (2010) 20: 6394-9 [PMID:20932747]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]