SB 224289 [Ligand Id: 130] activity data from GtoPdb and ChEMBL
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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 |
|---|---|---|---|---|---|---|---|---|
| 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 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]
