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ChEMBL ligand: CHEMBL281350 (SB-224289) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140] | ||||||||
ChEMBL | Compound was tested for binding affinity against Alpha-1A adrenergic receptor (rat submaxillary gland) | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1998) 41: 1218-1235 [PMID:9548813] |
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823] | ||||||||
ChEMBL | Compound was tested for binding affinity against Alpha-1B adrenergic receptor (rat liver, [3H] prazosin) | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1998) 41: 1218-1235 [PMID:9548813] |
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
ChEMBL | Compound was tested for binding affinity against human cloned Alpha-2A adrenergic receptor | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1998) 41: 1218-1235 [PMID:9548813] |
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2405] [GtoPdb: 26] [UniProtKB: P30545] | ||||||||
ChEMBL | Compound was tested for binding affinity against Alpha-2B adrenergic receptor (NG 108-15 cells) using [3H]RX-821002) as radioligand | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1998) 41: 1218-1235 [PMID:9548813] |
β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588] | ||||||||
ChEMBL | Compound was tested for binding affinity against human cloned Beta-1 adrenergic receptor | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1998) 41: 1218-1235 [PMID:9548813] |
β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550] | ||||||||
ChEMBL | Compound was tested for binding affinity against human cloned Beta-2 adrenergic receptor | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1998) 41: 1218-1235 [PMID:9548813] |
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
ChEMBL | Compound was tested for binding affinity against human cloned Dopamine receptor D2 | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1998) 41: 1218-1235 [PMID:9548813] |
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
ChEMBL | Compound was tested for binding affinity against human cloned Dopamine receptor D3 | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1998) 41: 1218-1235 [PMID:9548813] |
Histamine H1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3943] [UniProtKB: P31389] | ||||||||
ChEMBL | Compound was tested for binding affinity against Histamine H1 receptor. | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1998) 41: 1218-1235 [PMID:9548813] |
Histamine H2 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2882] [UniProtKB: P47747] | ||||||||
ChEMBL | Compound was tested for binding affinity towards Histamine H2 receptor | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1998) 41: 1218-1235 [PMID:9548813] |
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
ChEMBL | Compound was tested for binding affinity against human cloned Muscarinic acetylcholine receptor M1 | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1998) 41: 1218-1235 [PMID:9548813] |
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
ChEMBL | Compound was tested for binding affinity against human cloned Muscarinic acetylcholine receptor M2 | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1998) 41: 1218-1235 [PMID:9548813] |
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
ChEMBL | Compound was tested for binding affinity against human 5-hydroxytryptamine 1A receptor | B | 5.5 | pKi | >3162.28 | nM | Ki | J Med Chem (1998) 41: 1218-1235 [PMID:9548813] |
ChEMBL | Affinity for 5-hydroxytryptamine 1A receptor subtype | B | 6 | pKi | >1000 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 3183-3188 |
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
ChEMBL | Inhibition activity against 5-hydroxytryptamine 1A receptor in rat hippocampus membranes using radio binding assays | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2000) 43: 517-525 [PMID:10669578] |
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
ChEMBL | Affinity for 5-hydroxytryptamine 1B receptor subtype | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 3183-3188 |
ChEMBL | In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4786-4789 [PMID:16143528] |
ChEMBL | Binding affinity for human 5-hydroxytryptamine 1B receptor | B | 8.2 | pKi | 6.31 | nM | Ki | J Med Chem (1998) 41: 1218-1235 [PMID:9548813] |
GtoPdb | - | - | 8.6 | pKi | 2.51 | nM | Ki |
Br J Pharmacol (1998) 125: 202-8 [PMID:9776361]; Mol Pharmacol (2000) 58: 1042-9 [PMID:11040052]; J Med Chem (1998) 41: 1218-35 [PMID:9548813] |
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564] | ||||||||
ChEMBL | Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2000) 43: 517-525 [PMID:10669578] |
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
ChEMBL | Binding affinity for human 5-hydroxytryptamine 1D receptor | B | 6.3 | pKi | 501.19 | nM | Ki | J Med Chem (1998) 41: 1218-1235 [PMID:9548813] |
GtoPdb | - | - | 6.3 | pKi | - | - | - |
Br J Pharmacol (1998) 125: 202-8 [PMID:9776361]; J Med Chem (1998) 41: 1218-35 [PMID:9548813] |
ChEMBL | Affinity for 5-hydroxytryptamine 1D receptor subtype | B | 6.59 | pKi | 260 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 3183-3188 |
ChEMBL | Inhibition affinity against 5-HT-1D receptor in bovine caudate nucleus using radio binding assay | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2000) 43: 517-525 [PMID:10669578] |
5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566] | ||||||||
ChEMBL | Compound was tested for binding affinity against human 5-hydroxytryptamine 1E receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1998) 41: 1218-1235 [PMID:9548813] |
5-HT1F receptor/Serotonin 1f (5-HT1f) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1805] [GtoPdb: 5] [UniProtKB: P30939] | ||||||||
ChEMBL | Compound was tested for binding affinity against human 5-hydroxytryptamine 1F receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1998) 41: 1218-1235 [PMID:9548813] |
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
GtoPdb | - | - | 5.3 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733] |
ChEMBL | Binding affinity for human 5-hydroxytryptamine 2A receptor | B | 5.8 | pKi | 1584.89 | nM | Ki | J Med Chem (1998) 41: 1218-1235 [PMID:9548813] |
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
GtoPdb | - | - | 5.7 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733] |
ChEMBL | Compound was tested for binding affinity against human 5-hydroxytryptamine 2C receptor | B | 6.2 | pKi | 630.96 | nM | Ki | J Med Chem (1998) 41: 1218-1235 [PMID:9548813] |
GtoPdb | - | - | 6.2 | pKi | - | - | - | Br J Pharmacol (1998) 125: 202-8 [PMID:9776361] |
Serotonin 4 (5-HT4) receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2696] [UniProtKB: Q6Q253] | ||||||||
ChEMBL | Compound was tested for binding affinity against piglet hippocampus 5-hydroxytryptamine 4 receptor | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1998) 41: 1218-1235 [PMID:9548813] |
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
ChEMBL | Inhibition of 5-hydroxytryptamine reuptake | B | 5.33 | pIC50 | 4700 | nM | IC50 | J Med Chem (2000) 43: 517-525 [PMID:10669578] |
5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
GtoPdb | - | - | 5.9 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733] |
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]