dorsomorphin [Ligand Id: 4907] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL478629 (Dorsomorphin) |
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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: 1544, 1545, 1542, 1541, 1547, 1546, 1543] [UniProtKB: O43741, P54619, P54646, Q13131, Q9UGI9, Q9UGJ0, Q9Y478] | ||||||||
| 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
