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 | 68 | nM | IC50 | ACS Med Chem Lett (2023) 14: 833-840 [PMID:37312836] |
| 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 catalytic subunit alpha 1/protein kinase AMP-activated non-catalytic subunit gamma 1/protein kinase AMP-activated non-catalytic subunit beta 1/protein kinase AMP-activated catalytic subunit alpha 2/AMP-activated protein kinase, AMPK in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL4524016] [GtoPdb: 1541, 1545, 1543, 1542] [UniProtKB: D4A7E4, P54645, P80385, P80386, Q09137, Q6V7V4, Q9QZH4] | ||||||||
| ChEMBL | Inhibition of rat AMPK | B | 5.89 | pIC50 | 1280 | nM | IC50 | Eur J Med Chem (2022) 244: 114846-114846 [PMID:36283182] |
| 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] |
| ChEMBL | Inhibition of ALK3 (unknown origin) | B | 7.02 | pIC50 | 95 | nM | IC50 | ACS Med Chem Lett (2023) 14: 833-840 [PMID:37312836] |
| 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] |
| ChEMBL | Inhibition of ALK6 (unknown origin) | B | 6.63 | pIC50 | 235 | nM | IC50 | ACS Med Chem Lett (2023) 14: 833-840 [PMID:37312836] |
| 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] |
| ChEMBL | Inhibition of BMPR2 (unknown origin) | B | 7.13 | pIC50 | 74 | nM | IC50 | ACS Med Chem Lett (2023) 14: 833-840 [PMID:37312836] |
| 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 34:
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]
