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ChEMBL ligand: CHEMBL2051956 (Dexniguldipine, niguldipine, (r)-niguldipine) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]