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 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]
