LY134046 [Ligand Id: 6631] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL38681 (LY-134046) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL327] [GtoPdb: 25] [UniProtKB: P22909] | ||||||||
| ChEMBL | Inhibitory potency against alpha-2-adrenoceptor | B | 5.35 | pKi | 4500 | nM | Ki | J Med Chem (2004) 47: 37-44 [PMID:14695818] |
| Phenylethanolamine N-methyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4617] [GtoPdb: 2496] [UniProtKB: P11086] | ||||||||
| ChEMBL | Binding affinity to human PNMT K57A mutant | B | 4.04 | pKi | 90600 | nM | Ki | J Med Chem (2005) 48: 7243-7252 [PMID:16279783] |
| ChEMBL | Binding affinity to human PNMT V53A mutant | B | 4.65 | pKi | 22500 | nM | Ki | J Med Chem (2005) 48: 7243-7252 [PMID:16279783] |
| ChEMBL | Binding affinity to human wild type his-tagged PNMT | B | 5.36 | pKi | 4400 | nM | Ki | J Med Chem (2005) 48: 7243-7252 [PMID:16279783] |
| ChEMBL | Inhibitory constant against human phenylethanolamine N-methyl-transferase over-expressed in Escherichia coli | B | 6.55 | pKi | 280 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1579-1582 [PMID:11412985] |
| GtoPdb | - | - | 7.6 | pKi | - | - | - | Biochem Pharmacol (1981) 30: 1345-52 [PMID:6268095] |
| ChEMBL | Inhibitory binding affinity for phenylethanolamine N-methyl-transferase (PNMT) | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 4217-4220 [PMID:15261273] |
| Phenylethanolamine N-methyltransferase in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2331] [UniProtKB: P10938] | ||||||||
| ChEMBL | Affinity for bovine Phenylethanolamine N-Methyltransferase (PNMT) | B | 6.59 | pKi | 260 | nM | Ki | J Med Chem (1999) 42: 3588-3601 [PMID:10479290] |
| ChEMBL | Inhibition of PNMT (Phenylethanolamine N-Methyltransferase) in vitro | B | 6.59 | pKi | 260 | nM | Ki | J Med Chem (1999) 42: 3315-3323 [PMID:10464018] |
| ChEMBL | Inhibitory potency against bovine phenylethanolamine N-Methyltransferase (PNMT) | B | 6.59 | pKi | 260 | nM | Ki | J Med Chem (2004) 47: 37-44 [PMID:14695818] |
| ChEMBL | Ability to inhibit phenylethanolamine N-methyl-transferase (PNMT) | B | 6.59 | pKi | 260 | nM | Ki | J Med Chem (2001) 44: 2849-2856 [PMID:11495596] |
| ChEMBL | Inhibitory constant against bovine phenylethanolamine N-methyl-transferase | B | 6.66 | pKi | 220 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1579-1582 [PMID:11412985] |
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]
