intepirdine [Ligand Id: 9444] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1083390 (GSK-742457, GSK742457, Intepirdine, RVT-101, Sb-742457, SB-742457) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Displacement of [3H]-Raclopride from human dopamine D2L receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting method | B | 6 | pKi | 997 | nM | Ki | Eur J Med Chem (2018) 144: 716-729 [PMID:29291439] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5HT1AR expressed in HEK293 cell membranes after 1 hr by microbeta counting method | B | 5.63 | pKi | 2370 | nM | Ki | Eur J Med Chem (2018) 144: 716-729 [PMID:29291439] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Displacement of [3H]-Ketanserin from human 5HT2AR expressed in CHO-K1 cell membranes after 1.5 hrs by microbeta counting method | B | 7.59 | pKi | 26 | nM | Ki | Eur J Med Chem (2018) 144: 716-729 [PMID:29291439] |
| 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
| ChEMBL | Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells | B | 8 | pKi | <10 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 3214-3216 [PMID:19433358] |
| ChEMBL | Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2021) 64: 13279-13298 [PMID:34467765] |
| ChEMBL | Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr | B | 8.85 | pKi | 1.4 | nM | Ki | Bioorg Med Chem (2018) 26: 3588-3595 [PMID:29853337] |
| ChEMBL | Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2021) 64: 1180-1196 [PMID:33439019] |
| ChEMBL | Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method | B | 8.85 | pKi | 1.4 | nM | Ki | Eur J Med Chem (2018) 144: 716-729 [PMID:29291439] |
| ChEMBL | Binding affinity to 5HT6R (unknown origin) | B | 9.55 | pKi | 0.28 | nM | Ki | Eur J Med Chem (2018) 144: 716-729 [PMID:29291439] |
| ChEMBL | Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells | B | 9.6 | pKi | 0.25 | nM | Ki | J Med Chem (2014) 57: 7160-7181 [PMID:24850589] |
| ChEMBL | Binding affinity to 5HT6 receptor | B | 9.63 | pKi | 0.23 | nM | Ki | J Med Chem (2010) 53: 5186-5196 [PMID:20560595] |
| ChEMBL | Antagonist activity at 5-HT6 receptor (unknown origin) | B | 9.64 | pKi | 0.23 | nM | Ki | J Med Chem (2017) 60: 1843-1859 [PMID:28212021] |
| ChEMBL | Antagonist activity at 5-HT6 receptor (unknown origin) | B | 9.64 | pKi | 0.23 | nM | Ki | Bioorg Med Chem (2013) 21: 4614-4627 [PMID:23787290] |
| ChEMBL | Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis | B | 9.77 | pKi | 0.17 | nM | Ki | J Med Chem (2014) 57: 5823-5828 [PMID:24878269] |
| GtoPdb | HeLa cell membrane assay, displacing [3H]LSD | - | 9.77 | pKi | 0.17 | nM | Ki | J Med Chem (2014) 57: 5823-8 [PMID:24878269] |
| ChEMBL | Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis | B | 9.78 | pKi | 0.17 | nM | Ki | J Med Chem (2014) 57: 5823-5828 [PMID:24878269] |
| ChEMBL | Inverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assay | F | 7.01 | pIC50 | 97 | nM | IC50 | Eur J Med Chem (2020) 208: 112765-112765 [PMID:32949963] |
| ChEMBL | Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay | F | 8.55 | pIC50 | 2.8 | nM | IC50 | Eur J Med Chem (2018) 144: 716-729 [PMID:29291439] |
| ChEMBL | Inverse agonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as reduction in basal cAMP accumulation by BRET assay | F | 8.55 | pIC50 | 2.8 | nM | IC50 | J Med Chem (2021) 64: 1180-1196 [PMID:33439019] |
| ChEMBL | Antagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assay | F | 8.55 | pIC50 | 2.8 | nM | IC50 | J Med Chem (2021) 64: 13279-13298 [PMID:34467765] |
| 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3372] [GtoPdb: 11] [UniProtKB: P31388] | ||||||||
| ChEMBL | Displacement of [3H]Lu AE60157 from rat brain 5-HT6 receptor | B | 9.63 | pKi | 0.23 | nM | Ki | ACS Med Chem Lett (2016) 7: 618-622 [PMID:27326337] |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
| ChEMBL | Displacement of [3H]-5-CT from human 5HT7BR expressed in HEK293 cell membranes after 1 hr by microbeta counting method | B | 4.85 | pKi | 14230 | nM | Ki | Eur J Med Chem (2018) 144: 716-729 [PMID:29291439] |
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]
