S(+)-niguldipine [Ligand Id: 487] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL405355 ((+)-niguldipine, 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]
  • Alpha-1a adrenergic receptor in Bovine [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
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  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
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  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944]
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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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  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Rat [ChEMBL: CHEMBL3762] [GtoPdb: 529] [UniProtKB: P22002]
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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 Binding affinity against adenosine A1 receptor in rat cerebral cortex membrane by radioligand binding assay using [3H](R)-PIA. B 4 pKi >100000 nM Ki J. Med. Chem. (1996) 39: 4667-4675 [PMID:8917655]
ChEMBL Displacement of [3H]R-PIA from Adenosine A1 receptor of rat brain membrane B 4 pKi >100000 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 5 pKi <10000 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]
ChEMBL Displacement of [3H]-CGS- 21680 binding to Adenosine A2A receptor in rat striatal membranes B 5 pKi <10000 nM Ki J. Med. Chem. (1996) 39: 2980-2989 [PMID:8709132]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL Binding affinity against cloned human adenosine A3 receptor by radioligand binding assay using [125I]-AB-MECA. B 5.55 pKi 2800 nM Ki J. Med. Chem. (1996) 39: 4667-4675 [PMID:8917655]
ChEMBL Displacement of [125 I]AB-MECA from human Adenosine A3 receptor expressed in HEK cells B 5.55 pKi 2800 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 5.55 pKi 2800 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 Inhibition of [3H]prazosin binding to human Alpha-1A adrenergic receptor expressed in CHO cells B 8.74 pKi 1.8 nM Ki J. Med. Chem. (1995) 38: 3681-3716 [PMID:7562902]
ChEMBL Ability to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptor B 9.8 pKi 0.16 nM Ki J. Med. Chem. (1995) 38: 1579-1581 [PMID:7752182]
ChEMBL Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active B 9.8 pKi 0.16 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 657-664 [PMID:15664832]
GtoPdb - - 10 pKi - - - Br J Pharmacol (1997) 121: 1127-35 [PMID:9249248];
Mol Pharmacol (1995) 48: 250-8 [PMID:7651358]
Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
ChEMBL Binding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligand B 9.42 pKi 0.38 nM Ki J. Med. Chem. (1996) 39: 2253-2258 [PMID:8667368]
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL Binding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligand B 8.2 pKi 6.38 nM Ki J. Med. Chem. (1996) 39: 2253-2258 [PMID:8667368]
GtoPdb - - 9.3 pKi - - - J Biol Chem (2001) 276: 25366-71 [PMID:11331292]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
ChEMBL Inhibition of [3H]prazosin binding to human Alpha-1B adrenergic receptor expressed in CHO cells B 7.07 pKi 85 nM Ki J. Med. Chem. (1995) 38: 3681-3716 [PMID:7562902]
ChEMBL Ability to displace [3H]prazosin from cloned human Alpha-1B adrenergic receptor B 7.26 pKi 55 nM Ki J. Med. Chem. (1995) 38: 1579-1581 [PMID:7752182]
ChEMBL Binding affinity towards Alpha-1B adrenergic receptor hamster smooth muscle using [3H]prazosin as radioligand B 7.6 pKi 25.01 nM Ki J. Med. Chem. (1996) 39: 2253-2258 [PMID:8667368]
GtoPdb - - 7.7 pKi - - - Br J Pharmacol (1997) 121: 1127-35 [PMID:9249248];
Mol Pharmacol (1995) 48: 250-8 [PMID:7651358]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
ChEMBL Binding affinity towards Alpha-1B adrenergic receptor in rat liver using [3H]prazosin as radioligand B 6.42 pKi 379.9 nM Ki J. Med. Chem. (1996) 39: 2253-2258 [PMID:8667368]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL Inhibition of [3H]prazosin binding to human Alpha-1D adrenergic receptor expressed in CHO cells B 6.72 pKi 191 nM Ki J. Med. Chem. (1995) 38: 3681-3716 [PMID:7562902]
ChEMBL Ability to displace [3H]prazosin from cloned human Alpha-1D adrenergic receptor B 7 pKi 100 nM Ki J. Med. Chem. (1995) 38: 1579-1581 [PMID:7752182]
GtoPdb - - 7.4 pKi - - - Br J Pharmacol (1997) 121: 1127-35 [PMID:9249248];
Mol Pharmacol (1995) 48: 250-8 [PMID:7651358]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944]
ChEMBL Binding affinity towards Alpha-1D adrenergic receptor in rat brain using [3H]prazosin as radioligand B 7.08 pKi 82.41 nM Ki J. Med. Chem. (1996) 39: 2253-2258 [PMID:8667368]
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2A adrenergic receptor B 6.19 pKi 645 nM Ki J. Med. Chem. (1995) 38: 3681-3716 [PMID:7562902]
ChEMBL Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor B 6.28 pKi 530 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 Inhibition of [3H]rauwolscine binding to CHO cells expressing the human Alpha-2B adrenergic receptor B 5.3 pKi >5000 nM Ki J. Med. Chem. (1995) 38: 3681-3716 [PMID:7562902]
ChEMBL Ability to displace [3H]rauwolscine from cloned human Alpha-2B adrenergic receptor B 6.38 pKi 420 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 Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptor B 6.43 pKi 370 nM Ki J. Med. Chem. (1995) 38: 3681-3716 [PMID:7562902]
ChEMBL Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptor B 6.48 pKi 330 nM Ki J. Med. Chem. (1995) 38: 1579-1581 [PMID:7752182]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Binding affinity towards Dopamine receptor D2 in rat striatum using [3H]spiperone as radioligand B 6.53 pKi 294.9 nM Ki J. Med. Chem. (1996) 39: 2253-2258 [PMID:8667368]
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL Inhibition of P-glycoprotein-mediated daunorubicin efflux from human CCRF-CEM/VCR1000 cells after 240 secs by FACS flow cytometric analysis B 6.15 pIC50 707.95 nM IC50 J. Med. Chem. (2012) 55: 3261-3273 [PMID:22452412]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Binding affinity towards 5-hydroxytryptamine 1A receptor in rat hypocampus membrane using [3H]8-OH-DPAT as radioligand B 5 pKi >10000 nM Ki J. Med. Chem. (1996) 39: 2253-2258 [PMID:8667368]
Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3762] [GtoPdb: 529] [UniProtKB: P22002]
ChEMBL Inhibition of [3H]nitrendipine binding to membrane homogenates of of rat cardiac muscle. B 8.05 pKi 9 nM Ki J. Med. Chem. (1995) 38: 3681-3716 [PMID:7562902]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]