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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 |
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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]