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

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: CHEMBL281350 (SB-224289)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
There should be some charts here, you may need to enable JavaScript!
  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
There should be some charts here, you may need to enable JavaScript!
  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
There should be some charts here, you may need to enable JavaScript!
  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Mouse [ChEMBL: CHEMBL2405] [GtoPdb: 26] [UniProtKB: P30545]
There should be some charts here, you may need to enable JavaScript!
  • β1-adrenoceptor/Beta-1 adrenergic receptor in Human [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
There should be some charts here, you may need to enable JavaScript!
  • β2-adrenoceptor/Beta-2 adrenergic receptor in Human [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
There should be some charts here, you may need to enable JavaScript!
  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
There should be some charts here, you may need to enable JavaScript!
  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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!
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
There should be some charts here, you may need to enable JavaScript!
  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
There should be some charts here, you may need to enable JavaScript!
  • 5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT1F receptor/Serotonin 1f (5-HT1f) receptor in Human [ChEMBL: CHEMBL1805] [GtoPdb: 5] [UniProtKB: P30939]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
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
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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]