dexniguldipine [Ligand Id: 463] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2051956 (Dexniguldipine, Dexniguldipino, niguldipine, (r)-niguldipine)
  • A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
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  • A2A receptor/Adenosine A2a receptor in Rat [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
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  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
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  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
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  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
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  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
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  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
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  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL Displacement of [3H]R-PIA from Adenosine A1 receptor of rat brain membrane B 4.38 pKi 41300 nM Ki J Med Chem (1999) 42: 3055-3065 [PMID:10447949]
ChEMBL Displacement of [3H](R)-PIA binding to Adenosine A1 receptor in rat brain membranes B 4.38 pKi 41300 nM Ki J Med Chem (1996) 39: 2980-2989 [PMID:8709132]
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
ChEMBL Displacement of [3H]CGS-21680 from Adenosine A2A receptor of rat striatal membrane at 10e-4 uM B 4 pKi >100000 nM Ki J Med Chem (1999) 42: 3055-3065 [PMID:10447949]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
GtoPdb - - 5.7 pKi - - - J Med Chem (1996) 39: 2980-9 [PMID:8709132]
ChEMBL Displacement of [125 I]AB-MECA from human Adenosine A3 receptor expressed in HEK cells B 5.72 pKi 1900 nM Ki J Med Chem (1999) 42: 3055-3065 [PMID:10447949]
ChEMBL Displacement of [125]AB-MECA binding to human Adenosine A3 receptor expressed in HEK cells B 5.72 pKi 1900 nM Ki J Med Chem (1996) 39: 2980-2989 [PMID:8709132]
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
ChEMBL Ability to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptor B 8.33 pKi 4.7 nM Ki J Med Chem (1995) 38: 1579-1581 [PMID:7752182]
ChEMBL Binding affinity was tested on human Alpha-1A adrenergic receptor B 9.7 pKi 0.2 nM Ki J Med Chem (1997) 40: 1293-1315 [PMID:9135028]
ChEMBL Binding affinity was tested on human Alpha-1A adrenergic receptor B 9.8 pKi 0.16 nM Ki J Med Chem (1997) 40: 1293-1315 [PMID:9135028]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
ChEMBL Ability to displace [3H]prazosin from cloned human Alpha-1B adrenergic receptor B 7.25 pKi 56 nM Ki J Med Chem (1995) 38: 1579-1581 [PMID:7752182]
ChEMBL Binding affinity was tested on human Alpha-1B adrenergic receptor B 7.26 pKi 54.95 nM Ki J Med Chem (1997) 40: 1293-1315 [PMID:9135028]
ChEMBL Binding affinity was tested on human Alpha-1B adrenergic receptor B 7.6 pKi 25.12 nM Ki J Med Chem (1997) 40: 1293-1315 [PMID:9135028]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL Ability to displace [3H]prazosin from cloned human Alpha-1D adrenergic receptor B 6.77 pKi 170 nM Ki J Med Chem (1995) 38: 1579-1581 [PMID:7752182]
ChEMBL Binding affinity was tested on human Alpha-1D adrenergic receptor B 7 pKi 100 nM Ki J Med Chem (1997) 40: 1293-1315 [PMID:9135028]
ChEMBL Binding affinity was tested on human Alpha-1D adrenergic receptor B 7.1 pKi 79.43 nM Ki J Med Chem (1997) 40: 1293-1315 [PMID:9135028]
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor B 6.05 pKi 900 nM Ki J Med Chem (1995) 38: 1579-1581 [PMID:7752182]
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL Ability to displace [3H]rauwolscine from cloned human Alpha-2B adrenergic receptor B 6.18 pKi 660 nM Ki J Med Chem (1995) 38: 1579-1581 [PMID:7752182]
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptor B 6.35 pKi 450 nM Ki J Med Chem (1995) 38: 1579-1581 [PMID:7752182]
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in CEM/VLB100 cells F 5.64 pKi 2300 nM Ki Biochem Biophys Res Commun (1999) 257: 410-413 [PMID:10198227]
ChEMBL Compound was tested for inhibition of daunomycin efflux in the resistant human T-lymphoblast cell line CEM vcr1000. F 7.22 pEC50 60 nM EC50 J Med Chem (1998) 41: 4001-4011 [PMID:9767638]

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]