Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL1162395 |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
---|---|---|---|---|---|---|---|---|
Acetylcholine-binding protein in Lymnaea stagnalis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6084] [UniProtKB: P58154] | ||||||||
ChEMBL | Displacement of [3H]-epibatidine from Lymnaea stagnalis N-terminal FLAG-tagged AChBP expressed in HEK293 cells after 2 hrs by liquid scintillation counting | B | 9.4 | pKd | 0.4 | nM | Kd | Eur J Med Chem (2011) 46: 5625-5635 [PMID:21986237] |
nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α3 subunit/Neuronal acetylcholine receptor; alpha3/beta4 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907594] [GtoPdb: 474, 464] [UniProtKB: P30926, P32297] | ||||||||
ChEMBL | Displacement of [3H]-epibatidine from alpha3beta4 nAChR in human SH-SY5Y cellular membranes after 2 hrs by liquid scintillation counting | B | 6.01 | pKi | 970 | nM | Ki | Eur J Med Chem (2011) 46: 5625-5635 [PMID:21986237] |
ChEMBL | Displacement of [3H]epibatidine from human alpha3beta4 nAchR expressed in SH-SY5Y cells | B | 6.01 | pKi | 970 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1179-1186 [PMID:22177081] |
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]epibatidine from human alpha4beta2 nAchR expressed in SH-EP1 cells | B | 7.72 | pKi | 19 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1179-1186 [PMID:22177081] |
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]cytisine from alpha4beta2 nAChR in rat brain membrane after 3 hrs | B | 1.16 | pKi | 1.16 | uM | pKi | Eur J Med Chem (2010) 45: 2433-2446 [PMID:20236734] |
ChEMBL | Displacement of [3H]cytisine from alpha4beta2 nAChR in rat brain membrane after 3 hrs | B | 7.15 | pKi | 70 | nM | Ki | Eur J Med Chem (2010) 45: 2433-2446 [PMID:20236734] |
ChEMBL | Displacement of [3H]-epibatidine from alpha4beta2 nAChR in rat cortical membranes after 2 hrs by liquid scintillation counting | B | 7.72 | pKi | 19 | nM | Ki | Eur J Med Chem (2011) 46: 5625-5635 [PMID:21986237] |
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 [125I]alpha-bungarotoxin from alpha7 nAChR | B | 7.64 | pKd | 23 | nM | Kd | J Med Chem (2008) 51: 6293-6302 [PMID:18826295] |
ChEMBL | Agonist activity at human cloned wild-type alpha7 nAChR expressed in Xenopus laevis oocytes assessed as channel opening by voltage clamp electrophysiology | F | 5.52 | pEC50 | 3000 | nM | EC50 | J Med Chem (2008) 51: 6293-6302 [PMID:18826295] |
nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4980] [GtoPdb: 468] [UniProtKB: Q05941] | ||||||||
ChEMBL | Displacement of [125I]-alpha-bungarotoxin from alpha7 nAChR in rat brain membrane after 3 hrs | B | 0.62 | pKi | 0.62 | uM | pKi | Eur J Med Chem (2010) 45: 2433-2446 [PMID:20236734] |
ChEMBL | Displacement of [3H]-methyllycaconitine from alpha7 nAChR in rat hippocampal membranes after 2 hrs by liquid scintillation counting | B | 6.38 | pKi | 420 | nM | Ki | Eur J Med Chem (2011) 46: 5625-5635 [PMID:21986237] |
GtoPdb | Displacement of [3H]-methyllycaconitine from rat α7 nAChR in hippocampal membranes by liquid scintillation counting | - | 6.38 | pKi | 420 | nM | Ki | Eur J Med Chem (2011) 46: 5625-35 [PMID:21986237] |
ChEMBL | Displacement of [125I]-alpha-bungarotoxin from alpha7 nAChR in rat brain membrane after 3 hrs | B | 6.62 | pKi | 240 | nM | Ki | Eur J Med Chem (2010) 45: 2433-2446 [PMID:20236734] |
ChEMBL | Agonist activity at rat recombinant alpha7 nAChR expressed in GH4C1 cells by patch clamp technique | F | 5.8 | pEC50 | 1600 | nM | EC50 | Eur J Med Chem (2011) 46: 5625-5635 [PMID:21986237] |
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]