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

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ChEMBL ligand: CHEMBL2051956 (Dexniguldipine, 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 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]