SB 206553 [Ligand Id: 189] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL297784 (SB-206553)
  • A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Human [ChEMBL: CHEMBL2492] [GtoPdb: 468] [UniProtKB: P36544]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Rat [ChEMBL: CHEMBL323] [GtoPdb: 7] [UniProtKB: P30994]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Mouse [ChEMBL: CHEMBL3006] [GtoPdb: 8] [UniProtKB: P34968]
  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
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  • 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL Binding affinity against rat Adenosine A1 receptor B 4.3 pKi <50118.72 nM Ki J Med Chem (1995) 38: 2524-2530 [PMID:7629791]
CYP19A1/Cytochrome P450 19A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1978] [GtoPdb: 1362] [UniProtKB: P11511]
ChEMBL Inhibition of heterologously expressed human Cytochrome P450 19A1 at 100 uM B 4 pIC50 >100000 nM IC50 J Med Chem (1997) 40: 3494-3496 [PMID:9357513]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Binding affinity against human Dopamine receptor D2 expressed in CHO cells using [125I]iodosulpiride B 5 pKi <10000 nM Ki J Med Chem (1995) 38: 2524-2530 [PMID:7629791]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Binding affinity human Dopamine receptor D3 expressed in CHO cells using [125I]iodosulpiride B 5 pKi <10000 nM Ki J Med Chem (1995) 38: 2524-2530 [PMID:7629791]
Histamine H1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3943] [UniProtKB: P31389]
ChEMBL Binding affinity against guinea pig H1 receptor B 5 pKi <10000 nM Ki J Med Chem (1995) 38: 2524-2530 [PMID:7629791]
nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2492] [GtoPdb: 468] [UniProtKB: P36544]
ChEMBL Agonist activity at human alpha7 nAChR expressed in GH4C1 cells assessed as potentiation of nicotine-induced calcium signal F 5.82 pEC50 1500 nM EC50 J Med Chem (2011) 54: 7943-7961 [PMID:21919481]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Binding affinity against rat 5-hydroxytryptamine 1A receptor B 5 pKi <10000 nM Ki J Med Chem (1995) 38: 2524-2530 [PMID:7629791]
Serotonin 1d (5-HT1d) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304407] [UniProtKB: Q60484]
ChEMBL Binding affinity against guinea pig 5-hydroxytryptamine 1D receptor B 6 pKi <1000 nM Ki J Med Chem (1995) 38: 2524-2530 [PMID:7629791]
5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
ChEMBL Binding affinity against human 5-hydroxytryptamine 1E receptor expressed in CHO cells B 5.3 pKi <5011.87 nM Ki J Med Chem (1995) 38: 2524-2530 [PMID:7629791]
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 5-hydroxytryptamine 2A receptor expressed in HEK 293 cells B 5.7 pKi 1995.26 nM Ki J Med Chem (1997) 40: 3494-3496 [PMID:9357513]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 2A receptor expressed in HEK 293 cells using [3H]ketanserin as radioligand B 5.7 pKi 1995.26 nM Ki J Med Chem (1998) 41: 1598-1612 [PMID:9572885]
ChEMBL Binding affinity against human 5-hydroxytryptamine 2A receptor expressed in 293 cells using [3H]ketanserin B 5.79 pKi 1621.81 nM Ki J Med Chem (1995) 38: 2524-2530 [PMID:7629791]
ChEMBL Binding affinity analysed on 5-HT 2A human clone using [3H]ketanserin as radioligand B 5.79 pKi 1621.81 nM Ki J Med Chem (1996) 39: 2773-2780 [PMID:8709108]
GtoPdb - - 5.8 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733];
Br J Pharmacol (1996) 117: 427-434 [PMID:8821530]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
ChEMBL Displacement of [3H]ketanserin from 5-HT2A receptor of rat frontal cortex B 6.3 pKi 501.19 nM Ki J Med Chem (1996) 39: 4966-4977 [PMID:8960557]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL Binding affinity towards cloned human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT as radioligand B 7.6 pKi 25.12 nM Ki J Med Chem (1998) 41: 1598-1612 [PMID:9572885]
ChEMBL Displacement of [3H]5-HT from 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells B 7.6 pKi 25.12 nM Ki J Med Chem (1997) 40: 3494-3496 [PMID:9357513]
ChEMBL Displacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting method B 7.65 pKi 22.2 nM Ki Medchemcomm (2018) 9: 1069-1075 [PMID:30108996]
ChEMBL Displacement of [3H]LSD from human recombinant 5-HT2B receptor stably expressed in HEK cell membrane after 90 mins by scintillation counting method B 7.68 pKi 21 nM Ki Medchemcomm (2015) 6: 601-605
ChEMBL Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) B 7.92 pKi 12.02 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL Displacement of [3H]LSD from 5-HT2B receptor (unknown origin) B 7.92 pKi 12 nM Ki Bioorg Med Chem Lett (2014) 24: 576-579 [PMID:24365159]
ChEMBL Displacement of [3H]LSD from human cloned 5HT2B receptor expressed in CHO cells by liquid scintillation counting B 8.37 pKi 4.3 nM Ki J Med Chem (2010) 53: 7573-7586 [PMID:20958049]
GtoPdb - - 8.5 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733];
Br J Pharmacol (2004) 143: 549-60 [PMID:15466450]
ChEMBL Antagonist activity at recombinant human 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced increase in inositol1-phosphate accumulation measured after 30 mins by HTRF assay F 7.89 pEC50 13 nM EC50 J Med Chem (2020) 63: 5526-5567 [PMID:32342685]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL323] [GtoPdb: 7] [UniProtKB: P30994]
ChEMBL Inhibitory potency against rat stomach fundus 5-hydroxytryptamine 2B receptor B 8.48 pKd 3.31 nM Kd J Med Chem (1995) 38: 2524-2530 [PMID:7629791]
ChEMBL Inhibition of 5-HT binding to 5-HT2B receptor of Rat stomach fundus B 8.5 pKd 3.16 nM Kd J Med Chem (1996) 39: 4966-4977 [PMID:8960557]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Displacement of [3H]mesulergine from 5-hydroxytryptamine 2C receptor expressed in HEK 293 cells B 7.9 pKi 12.59 nM Ki J Med Chem (1997) 40: 3494-3496 [PMID:9357513]
ChEMBL Binding affinity towards cloned human 5-hydroxytryptamine 2C receptor expressed in HEK 293 cells using [3H]mesulergine as radioligand B 7.9 pKi 12.59 nM Ki J Med Chem (1998) 41: 1598-1612 [PMID:9572885]
GtoPdb - - 7.9 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733];
Br J Pharmacol (1996) 117: 427-434 [PMID:8821530]
ChEMBL Binding affinity against human 5-hydroxytryptamine 2C receptor expressed in 293 cells using [3H]mesulergine B 8 pKi 10 nM Ki J Med Chem (1995) 38: 2524-2530 [PMID:7629791]
ChEMBL Displacement of [3H]LSD from human recombinant 5-HT2C receptor expressed in HEK cells by radioligand completion assay relative to control B 8.55 pKi 2.8 nM Ki J Med Chem (2021) 64: 13510-13523 [PMID:34467758]
ChEMBL Antagonist activity at human recombinant 5-HT2C receptor assessed as inhibition of serotonin-induced inositol phosphate accumulation F 8.03 pIC50 9.4 nM IC50 J Med Chem (2014) 57: 4543-4557 [PMID:24805037]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3006] [GtoPdb: 8] [UniProtKB: P34968]
ChEMBL Binding affinity analysed on 5-HT 2C in human clone using [3H]mesulergine as radioligand B 8 pKi 10 nM Ki J Med Chem (1996) 39: 2773-2780 [PMID:8709108]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
ChEMBL Displacement of [3H]mesulergine from rat 5-HT2C receptor expressed in HEK293 B 8.3 pKi 5.01 nM Ki J Med Chem (1996) 39: 4966-4977 [PMID:8960557]
5-HT3A/5-HT3B/Serotonin 3 (5-HT3) receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094116] [GtoPdb: 373, 374] [UniProtKB: P35563, Q9JJ16]
ChEMBL Binding affinity against rat 5-hydroxytryptamine 3 receptor B 5 pKi <10000 nM Ki J Med Chem (1995) 38: 2524-2530 [PMID:7629791]
5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758]
ChEMBL Binding affinity against rat 5-hydroxytryptamine 4 receptor B 5.3 pKi 5011.87 nM Ki J Med Chem (1995) 38: 2524-2530 [PMID:7629791]

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]