DHβE [Ligand Id: 4006] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL293950 (Dihydro-Beta-Erythroidine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor β4 subunit/Neuronal acetylcholine receptor; alpha3/beta4 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907593] [GtoPdb: 464, 474] [UniProtKB: P04757, P12392] | ||||||||
| ChEMBL | Displacement of [3H]epibatidine from rat alpha3beta4 nAChR transfected in HEK293 cells after 4 hrs by scintillation count analysis | B | 4 | pKi | 100000 | nM | Ki | ACS Med Chem Lett (2014) 5: 766-770 [PMID:25050162] |
| ChEMBL | Activity at rat alpha3beta4 nicotinic receptor expressed in KXalpha-3-beta-4R2 cells assessed as nicotine-induced 86Rb+ efflux | B | 4 | pIC50 | 100000 | nM | IC50 | J Nat Prod (2006) 69: 1514-1516 [PMID:17067175] |
| ChEMBL | Antagonist activity at rat alpha3beta4 nAChR transfected in HEK293 cells by FLIPR membrane potential blue (FMP) assay | B | 4 | pIC50 | 100000 | nM | IC50 | ACS Med Chem Lett (2014) 5: 766-770 [PMID:25050162] |
| ChEMBL | Antagonist activity at rat alpha3beta4 nAChR | B | 4.64 | pIC50 | 23000 | nM | IC50 | J Med Chem (2014) 57: 8204-8223 [PMID:24901260] |
| nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor α4 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907589] [GtoPdb: 472, 465] [UniProtKB: P17787, P43681] | ||||||||
| ChEMBL | Displacement of [3H]cytisine from alpha4/beta2 nAChR (unknown origin) | B | 7.01 | pKi | 98 | nM | Ki | J Med Chem (2013) 56: 9673-9682 [PMID:24187998] |
| ChEMBL | Antagonist activity at (alpha4beta2)2beta2 nAChR (unknown origin) expressed in Xenopus oocytes assessed as inhibition of acetylcholine-induced current after 2 mins by two-electrode voltage clamp assay | B | 6.39 | pIC50 | 410 | nM | IC50 | Bioorg Med Chem (2013) 21: 2687-2694 [PMID:23561269] |
| ChEMBL | Antagonist activity at (alpha4beta2)2alpha4 nAChR (unknown origin) expressed in Xenopus oocytes assessed as inhibition of acetylcholine-induced current after 2 mins by two-electrode voltage clamp assay | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem (2013) 21: 2687-2694 [PMID:23561269] |
| nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor β2 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907596] [GtoPdb: 465, 472] [UniProtKB: P09483, P12390] | ||||||||
| ChEMBL | Displacement of [3H]epibatidine from rat alpha4beta2 nAChR transfected in HEK293 cells after 4 hrs by scintillation count analysis | B | 6.09 | pKi | 820 | nM | Ki | ACS Med Chem Lett (2014) 5: 766-770 [PMID:25050162] |
| ChEMBL | Inhibition of rat membrane alpha4beta2 nAChR by [3H]cytisine binding assay | B | 6.85 | pKi | 140 | nM | Ki | ACS Med Chem Lett (2014) 5: 766-770 [PMID:25050162] |
| ChEMBL | Antagonist activity at rat alpha4beta2 nAChR | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2014) 57: 8204-8223 [PMID:24901260] |
| nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor β4 subunit/Neuronal acetylcholine receptor; alpha4/beta4 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907595] [GtoPdb: 465, 474] [UniProtKB: P09483, P12392] | ||||||||
| ChEMBL | Displacement of [3H]epibatidine from rat alpha4beta4 nAChR transfected in HEK293 cells after 4 hrs by scintillation count analysis | B | 4 | pKi | 100000 | nM | Ki | ACS Med Chem Lett (2014) 5: 766-770 [PMID:25050162] |
| nicotinic acetylcholine receptor α4 subunit/Neuronal acetylcholine receptor protein alpha-4 subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL307] [GtoPdb: 465] [UniProtKB: P09483] | ||||||||
| ChEMBL | Blockade of Nicotinic acetylcholine receptor alpha4-beta2 | B | 8.44 | pIC50 | 3.66 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1879-1887 [PMID:15050620] |
| nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2492] [GtoPdb: 468] [UniProtKB: P36544] | ||||||||
| ChEMBL | Displacement of [3H]cytisine from alpha7 nAChR (unknown origin) | B | 4.98 | pKi | 10500 | nM | Ki | J Med Chem (2013) 56: 9673-9682 [PMID:24187998] |
| nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor β2 subunit/Nicotinic acetylcholine receptor alpha-4/beta-2 in Mouse (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3301382] [GtoPdb: 474, 472] [UniProtKB: Q8R493, Q9ERK7] | ||||||||
| ChEMBL | Antagonist activity at mouse alpha4beta2 nAChR transfected in HEK293 cells by FLIPR membrane potential blue (FMP) assay | B | 5.92 | pIC50 | 1200 | nM | IC50 | ACS Med Chem Lett (2014) 5: 766-770 [PMID:25050162] |
| nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor α5 subunit/nicotinic acetylcholine receptor α4 subunit/Nicotinic acetylcholine receptor alpha4/beta2/alpha5 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038461] [GtoPdb: 472, 466, 465] [UniProtKB: P17787, P30532, P43681] | ||||||||
| ChEMBL | Antagonist activity at (alpha4beta2)2alpha5 nAChR (unknown origin) expressed in Xenopus oocytes assessed as inhibition of acetylcholine-induced current after 2 mins by two-electrode voltage clamp assay | B | 7.96 | pIC50 | 11 | nM | IC50 | Bioorg Med Chem (2013) 21: 2687-2694 [PMID:23561269] |
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]
