milrinone [Ligand Id: 5225] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL189 (Milrila, Milrinona, Milrinone, NSC-760072, 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 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]
