SB 258719 [Ligand Id: 281] 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: CHEMBL12264 (SB-258719)
  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
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!
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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]
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-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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!
  • Serotonin 4 (5-HT4) receptor in Guinea pig [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
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
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
ChEMBL The compound was tested for its binding affinity towards adrenergic alpha-1B receptors B 4.8 pKi <15848.93 nM Ki J Med Chem (1998) 41: 655-657 [PMID:9513592]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL The compound was tested for its binding affinity towards cloned human Dopamine receptor D2 in CHO cells using [125I]iodosulpiride. B 5.4 pKi 3981.07 nM Ki J Med Chem (1998) 41: 655-657 [PMID:9513592]
ChEMBL Displacement of [3H]raclopride from human dopamine receptor D2A expressed in mouse Ltk cells B 5.4 pKi 3981 nM Ki J Med Chem (2001) 44: 1337-1340 [PMID:11311055]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL The compound was tested for its binding affinity towards cloned human Dopamine receptor D3 in CHO cells using [125I]iodosulpiride. B 5.4 pKi 3981.07 nM Ki J Med Chem (1998) 41: 655-657 [PMID:9513592]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL The compound was tested for its binding affinity towards cloned human 5-hydroxytryptamine 1A receptor in HEK 293 cells using [3H]8-OH-DPAT. B 5.1 pKi <7943.28 nM Ki J Med Chem (1998) 41: 655-657 [PMID:9513592]
ChEMBL Displacement of [3H]8-OH-DPAT from human 5-hydroxytryptamine 1A receptor expressed in CHO cells B 5.1 pKi >7943 nM Ki J Med Chem (2001) 44: 1337-1340 [PMID:11311055]
ChEMBL Antagonist activity at 5-HT1A receptor (unknown origin) B 5.52 pKi >3000 nM Ki Eur J Med Chem (2019) 183: 111705-111705 [PMID:31581003]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
ChEMBL The compound was tested for its binding affinity towards cloned human 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT B 5.3 pKi <5011.87 nM Ki J Med Chem (1998) 41: 655-657 [PMID:9513592]
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
ChEMBL The compound was tested for its binding affinity towards cloned human 5-hydroxytryptamine 1D receptor in CHO cells using [3H]5-HT. B 5.5 pKi 3162.28 nM Ki J Med Chem (1998) 41: 655-657 [PMID:9513592]
5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
ChEMBL The compound was tested for its binding affinity towards cloned human 5-hydroxytryptamine 1E receptor in CHO cells using [3H]5-HT. B 4.8 pKi <15848.93 nM Ki J Med Chem (1998) 41: 655-657 [PMID:9513592]
5-HT1F receptor/Serotonin 1f (5-HT1f) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1805] [GtoPdb: 5] [UniProtKB: P30939]
ChEMBL The compound was tested for its binding affinity towards cloned human 5-hydroxytryptamine 1F receptor in CHO cells using [3H]5-HT. B 5.2 pKi <6309.57 nM Ki J Med Chem (1998) 41: 655-657 [PMID:9513592]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL The compound was tested for its binding affinity towards cloned human 5-hydroxytryptamine 2A receptor in HEK293 cells using [3H]-ketanserin. B 4.8 pKi <15848.93 nM Ki J Med Chem (1998) 41: 655-657 [PMID:9513592]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL The compound was tested for its binding affinity towards cloned human 5-hydroxytryptamine 2B receptors in HEK293 cells using [3H]5-HT. B 5.3 pKi <5011.87 nM Ki J Med Chem (1998) 41: 655-657 [PMID:9513592]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL The compound was tested for its binding affinity towards cloned human 5-hydroxytryptamine 2C receptor in HEK293 cells using [3H]mesulergine. B 4.8 pKi <15848.93 nM Ki J Med Chem (1998) 41: 655-657 [PMID:9513592]
Serotonin 4 (5-HT4) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
ChEMBL The compound was tested for its binding affinity towards 5-hydroxytryptamine 4 receptor in guinea pig hippocampus using [125I]SB-207710. B 5 pKi <10000 nM Ki J Med Chem (1998) 41: 655-657 [PMID:9513592]
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL The compound was tested for its binding affinity towards cloned human 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]5-LSD. B 4.8 pKi <15848.93 nM Ki J Med Chem (1998) 41: 655-657 [PMID:9513592]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 7 receptor B 7.49 pKi 32 nM Ki J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSD B 7.49 pKi 32 nM Ki Bioorg Med Chem Lett (2002) 12: 2451-2454 [PMID:12161155]
GtoPdb - - 7.5 pKi 31.6 nM Ki Br J Pharmacol (1998) 124: 1300-6 [PMID:9720804]
ChEMBL The compound was tested for its binding affinity towards cloned human 5-hydroxytryptamine 7 receptor expressed in HEK 293 cells using [3H]5-CT. B 7.5 pKi 31.62 nM Ki J Med Chem (1998) 41: 655-657 [PMID:9513592]
ChEMBL Binding affinity towards cloned human 5-hydroxytryptamine 7 receptor in HEK 293 cells B 7.5 pKi 31.62 nM Ki Bioorg Med Chem Lett (2000) 10: 1097-1100 [PMID:10843226]
ChEMBL The compound was tested for its binding affinity towards cloned human 5-hydroxytryptamine 7 receptor in HEK 293 cells using [3H]5-CT. B 7.5 pKi 31.62 nM Ki J Med Chem (1998) 41: 655-657 [PMID:9513592]
ChEMBL Binding affinity towards cloned human 5-hydroxytryptamine 7 receptor was determined in HEK293 cells using [3H]5-CT as radioligand B 7.5 pKi 31.62 nM Ki J Med Chem (2003) 46: 5638-5650 [PMID:14667218]
ChEMBL Binding affinity to 5HT7 receptor (unknown origin) B 7.5 pKi 31.6 nM Ki Bioorg Med Chem (2013) 21: 2568-2576 [PMID:23541835]
ChEMBL Binding affinity to 5-HT7 receptor (unknown origin) B 7.5 pKi 31.6 nM Ki J Med Chem (2018) 61: 8475-8503 [PMID:29767995]
ChEMBL Antagonist activity at 5-HT7 receptor (unknown origin) B 7.5 pKi 31.6 nM Ki Eur J Med Chem (2019) 183: 111705-111705 [PMID:31581003]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
ChEMBL Binding affinity towards 5-hydroxytryptamine receptor 7 on rat hypothalamus membranes using [3H]5-CT as radioligand. B 7.1 pKi 79.43 nM Ki J Med Chem (2003) 46: 5638-5650 [PMID:14667218]
ChEMBL Displacement of [3H]5-HT from rat 5-hydroxytryptamine 7 receptor expressed in CHO cells B 7.5 pKi 31.6 nM Ki J Med Chem (2001) 44: 1337-1340 [PMID:11311055]

ChEMBL data shown on this page come from version 32:

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]