milrinone [Ligand Id: 5225] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL189 (Milrila, Milrinone, NSC-760072, Primacor, WIN 47,203-2, WIN-47203-2) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| aurora kinase B/Aurora kinase B/Inner centromere protein in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3430907] [GtoPdb: 1937] [UniProtKB: Q96GD4, Q9NQS7] | ||||||||
| ChEMBL | Inhibition of human full length N-terminal GST-tagged Aurora B (1 to 344 end residues)/His-tagged INCENP (803 to 918 end residues) expressed in baculovirus expression system using fluorescence-labeled FL-Peptide 21 as substrate after 60 mins in presence of ATP by fluorescence assay based Cheng-Prusoff equation analysis | B | 4 | pKi | >100000 | nM | Ki | Bioorg Med Chem (2018) 26: 3021-3029 [PMID:29764757] |
| cAMP-specific 3`,5`-cyclic phosphodiesterase 4A in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366459] [UniProtKB: O89085] | ||||||||
| ChEMBL | Inhibition of Cavia porcellus (guinea pig) PDE3 isolated from heart using [3H]cAMP as substrate by two-step method | B | 5.33 | pKi | 4670 | nM | Ki | Med Chem Res (2008) 17: 587-603 |
| COX-1 /Cyclooxygenase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219] | ||||||||
| ChEMBL | Inhibition of thrombin-induced platelet aggregation | F | 5.33 | pIC50 | 4700 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 1080-1083 [PMID:16290144] |
| TTK protein kinase/Dual specificity protein kinase TTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3983] [GtoPdb: 2264] [UniProtKB: P33981] | ||||||||
| ChEMBL | Inhibition of full length human Mps1 using fluorescence-labeled H236 peptide as substrate after 60 to 90 mins in presence of ATP by fluorescence assay based Cheng-Prusoff equation analysis | B | 4 | pKi | >100000 | nM | Ki | Bioorg Med Chem (2018) 26: 3021-3029 [PMID:29764757] |
| phosphodiesterase 2A/Phosphodiesterase 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2652] [GtoPdb: 1297] [UniProtKB: O00408] | ||||||||
| ChEMBL | Inhibition of phosphodiesterase 2 (PDE2) from porcine platelets | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2000) 43: 2523-2529 [PMID:10891111] |
| GtoPdb | - | - | 6.52 | pIC50 | >300 | nM | IC50 | Biochem Pharmacol (2000) 59: 347-56 [PMID:10644042] |
| phosphodiesterase 3A/Phosphodiesterase 3A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL241] [GtoPdb: 1298] [UniProtKB: Q14432] | ||||||||
| ChEMBL | Inhibition of human recombinant PDE3A assessed as cAMP hydrolysis after 60 mins by fluorescence polarization assay using fluorescein-tagged cAMP as substrate | B | 4.94 | pIC50 | 11400 | nM | IC50 | Bioorg Med Chem (2009) 17: 5974-5982 [PMID:19628397] |
| ChEMBL | Inhibition of human recombinant PDE3A assessed as cGMP hydrolysis after 60 mins by fluorescence polarization assay using tetramethylrhodamine-tagged cGMP as substrate | B | 5.44 | pIC50 | 3600 | nM | IC50 | Bioorg Med Chem (2009) 17: 5974-5982 [PMID:19628397] |
| ChEMBL | Inhibitory concentration required to inhibit human phosphodiesterase 3A expressed in Escherichia coli | B | 6.36 | pIC50 | 440 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 3983-3987 [PMID:14592490] |
| GtoPdb | - | - | 6.36 | pIC50 | 440 | nM | IC50 |
Biochem Pharmacol (2000) 59: 347-56 [PMID:10644042]; Bioorg Med Chem Lett (2003) 13: 3983-7 [PMID:14592490] |
| Phosphodiesterase 3A in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3061] [UniProtKB: Q9XSW7] | ||||||||
| ChEMBL | Inhibition of phosphodiesterase 3 (PDE3) from porcine platelets, range 0.581-1.23 | B | 6.07 | pIC50 | 843 | nM | IC50 | J Med Chem (2000) 43: 2523-2529 [PMID:10891111] |
| phosphodiesterase 3B/Phosphodiesterase 3B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL290] [GtoPdb: 1299] [UniProtKB: Q13370] | ||||||||
| GtoPdb | - | - | 6 | pIC50 | 1000 | nM | IC50 | Biochem Pharmacol (2000) 59: 347-56 [PMID:10644042] |
| ChEMBL | Inhibitory concentration required to inhibit human phosphodiesterase 3B expressed in Escherichia coli | B | 6.55 | pIC50 | 280 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 3983-3987 [PMID:14592490] |
| Phosphodiesterase 3B in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5129] [UniProtKB: E1BN64] | ||||||||
| ChEMBL | Inhibition of bovine arterial Phosphodiesterase 3 | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (1996) 39: 297-303 [PMID:8568820] |
| Phosphodiesterase 4A in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3333] [UniProtKB: O77823] | ||||||||
| ChEMBL | Inhibition of phosphodiesterase 4 (PDE4) from porcine liver, range 10.4-16.3 | B | 4.89 | pIC50 | 13000 | nM | IC50 | J Med Chem (2000) 43: 2523-2529 [PMID:10891111] |
| phosphodiesterase 5A/Phosphodiesterase 5A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1827] [GtoPdb: 1304] [UniProtKB: O76074] | ||||||||
| ChEMBL | 50% inhibitory concentration against phosphodiesterase 5 (PDE5) from porcine platelets | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2000) 43: 2523-2529 [PMID:10891111] |
| ChEMBL | Inhibitory activity against cGMP-phosphodiesterase from porcine aorta | B | 6.13 | pIC50 | 740 | nM | IC50 | J Med Chem (1994) 37: 2106-2111 [PMID:8027992] |
| GtoPdb | - | - | 7.31 | pIC50 | 49.1 | nM | IC50 | |
| Phosphodiesterase 5A in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3478] [UniProtKB: Q28156] | ||||||||
| ChEMBL | Inhibition of bovine arterial Phosphodiesterase 5 | B | 5.3 | pIC50 | 5000 | nM | IC50 | J Med Chem (1996) 39: 297-303 [PMID:8568820] |
| phosphodiesterase 5A/Phosphodiesterase 5A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4567] [GtoPdb: 1304] [UniProtKB: O54735] | ||||||||
| ChEMBL | Inhibition of Phosphodiesterase 5 | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (1997) 7: 89-94 |
| aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965] | ||||||||
| ChEMBL | Inhibition of full length N-terminal His-tagged Aurora A (unknown origin) using fluorescence-labeled FL-Peptide 21 as substrate after 60 mins in presence of ATP by fluorescence assay based Cheng-Prusoff equation analysis | B | 4 | pKi | >100000 | nM | Ki | Bioorg Med Chem (2018) 26: 3021-3029 [PMID:29764757] |
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]
