fenoldopam [Ligand Id: 939] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL588 (Carlacor, Fenoldopam, SK-82526, SK&F-82526)
  • A2B receptor/Adenosine A2b receptor in Rat [ChEMBL: CHEMBL2592] [GtoPdb: 20] [UniProtKB: P29276]
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  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
  • D1 receptor/Dopamine D1 receptor in Rat [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • Dopamine D2 receptor in Bovine [ChEMBL: CHEMBL3998] [UniProtKB: P20288]
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • lysine demethylase 4E/Lysine-specific demethylase 4D-like in Human [ChEMBL: CHEMBL1293226] [GtoPdb: 2679] [UniProtKB: B2RXH2]
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  • lysine demethylase 1A/Lysine-specific histone demethylase 1 in Human [ChEMBL: CHEMBL6136] [GtoPdb: 2669] [UniProtKB: O60341]
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  • D4 receptor in Human [GtoPdb: 217] [UniProtKB: P21917]
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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
lysine demethylase 1A/Lysine-specific histone demethylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6136] [GtoPdb: 2669] [UniProtKB: O60341]
ChEMBL Inhibition of LSD1 (unknown origin) B 6.05 pIC50 890 nM IC50 Eur J Med Chem (2022) 228: 114042-114042 [PMID:34915312]
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 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]