S(+)-niguldipine [Ligand Id: 487] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL405355 ((+)-niguldipine, Niguldipine) |
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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]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144] |
| 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]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144] |
| 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]; Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144] |
| 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 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]
