fenoldopam [Ligand Id: 939] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL588 (Carlacor, Fenoldopam, SK-82526, SK&F-82526) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| A2B receptor/Adenosine A2b receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2592] [GtoPdb: 20] [UniProtKB: P29276] | ||||||||
| ChEMBL | Compound was tested for its binding affinity against Alpha-2 adrenergic receptor | B | 7.45 | pKi | 35.48 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 2371-2376 |
| D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
| ChEMBL | Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells | B | 7.55 | pKd | 28 | nM | Kd | J Med Chem (1996) 39: 850-859 [PMID:8632409] |
| ChEMBL | Affinity towards Dopamine receptor D1 | B | 7.4 | pKi | 40 | nM | Ki | J Med Chem (1998) 41: 4385-4399 [PMID:9784114] |
| GtoPdb | - | - | 7.9 | pKi | - | - | - | J Biol Chem (1994) 269: 27925-31 [PMID:7525564] |
| ChEMBL | Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay | B | 7.5 | pEC50 | 31.7 | nM | EC50 | J Med Chem (2018) 61: 9841-9878 [PMID:29939744] |
| ChEMBL | Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay | F | 8.55 | pEC50 | 2.8 | nM | EC50 | J Med Chem (2018) 61: 9841-9878 [PMID:29939744] |
| D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901] | ||||||||
| ChEMBL | Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes | B | 8.52 | pKi | 3 | nM | Ki | J Med Chem (1986) 29: 1904-1912 [PMID:3761310] |
| ChEMBL | Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390 | B | 8.91 | pKi | 1.23 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 2371-2376 |
| ChEMBL | Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes | F | 7.24 | pEC50 | 57 | nM | EC50 | J Med Chem (1987) 30: 1166-1176 [PMID:2955118] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Affinity towards Dopamine receptor D2 | B | 6.09 | pKi | 810 | nM | Ki | J Med Chem (1998) 41: 4385-4399 [PMID:9784114] |
| Dopamine D2 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3998] [UniProtKB: P20288] | ||||||||
| ChEMBL | Compound was tested for inhibition of [3H]spiroperidol binding against Dopamine receptor D2 | B | 6.1 | pKi | 790 | nM | Ki | J Med Chem (1986) 29: 1904-1912 [PMID:3761310] |
| ChEMBL | Displacement of [3H]spiroperidol from homogenized bovine pituitary Dopamine receptor D2 | B | 5.8 | pIC50 | 1580 | nM | IC50 | J Med Chem (1987) 30: 1166-1176 [PMID:2955118] |
| D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
| ChEMBL | In vitro affinity at mutant D2 receptor (S194A) in C6 (glioma) cell membranes. | B | 4.89 | pKd | 13000 | nM | Kd | J Med Chem (2000) 43: 3005-3019 [PMID:10956209] |
| ChEMBL | In vitro affinity at mutant D2 receptor (S194A) in C6 (glioma) cell membranes. | B | 5.57 | pKd | 2700 | nM | Kd | J Med Chem (2000) 43: 3005-3019 [PMID:10956209] |
| ChEMBL | In vitro affinity at mutant D2 receptor (S197A) in C6 (glioma) cell membranes. | B | 5.72 | pKd | 1900 | nM | Kd | J Med Chem (2000) 43: 3005-3019 [PMID:10956209] |
| ChEMBL | In vitro affinity at wild type Dopamine receptor D2 on C6 (glioma) cell membranes. | B | 5.89 | pKd | 1300 | nM | Kd | J Med Chem (2000) 43: 3005-3019 [PMID:10956209] |
| ChEMBL | Binding affinity against Dopamine receptor D2 in rat striatal membranes using [3H]spiperone | B | 7.88 | pKi | 13.18 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 2371-2376 |
| lysine demethylase 4E/Lysine-specific demethylase 4D-like in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293226] [GtoPdb: 2679] [UniProtKB: B2RXH2] | ||||||||
| ChEMBL | Non-competitive inhibition of JMJD2E relative to alpha-ketoglutarate | B | 5.72 | pKi | 1920 | nM | Ki | Bioorg Med Chem (2011) 19: 3625-3636 [PMID:21596573] |
| ChEMBL | Inhibition of N-terminal His-6-tagged human JMJD2E (1 to 337 residues) expressed in Escherichia coli by MALDI-TOF/MS analysis | B | 5.52 | pIC50 | 3000 | nM | IC50 | Medchemcomm (2012) 3: 135-161 |
| D4 receptor in Human [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
| GtoPdb | - | - | 6.5 | pKi | - | - | - | Nature (1991) 350: 610-4 [PMID:1840645] |
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]
