SB 204741 [Ligand Id: 221] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL323356 (SB-204741)
  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
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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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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
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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]
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  • 5-HT2B receptor in Human [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]
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  • 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL The binding affinity (pKi) measured against Dopamine receptor D1 using [3H]-SCH- 23390 as radioligand B 5 pKi <10000 nM Ki J. Med. Chem. (1995) 38: 855-857 [PMID:7699699]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL In vitro binding affinity was measured on Dopamine receptor D2 B 4.5 pKi <31622.78 nM Ki J. Med. Chem. (1995) 38: 855-857 [PMID:7699699]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL The binding affinity (pKi) measured against Dopamine receptor D3 (cloned human receptors in CHO cells) using [125I]iodosulpiride as radioligand B 4.5 pKi <31622.78 nM Ki J. Med. Chem. (1995) 38: 855-857 [PMID:7699699]
GABAA receptor π subunit/GABAA receptor β1 subunit/GABAA receptor δ subunit/GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor γ1 subunit/GABAA receptor α2 subunit/GABAA receptor α4 subunit/GABAA receptor γ3 subunit/GABAA receptor α6 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit/GABAA receptor β2 subunit/GABAA receptor ε subunit/GABA-A receptor; anion channel in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907607] [GtoPdb: 419, 410, 416, 414, 408, 406, 413, 405, 407, 415, 409, 404, 412, 411, 417] [UniProtKB: O09028, P15431, P18506, P18508, P19969, P20236, P23574, P23576, P28471, P28473, P30191, P62813, P63079, P63138, Q91ZM7, Q9ES14]
ChEMBL Inhibition of [3H]muscimol binding to Gamma-aminobutyric acid A (GABA-A) receptor of rat cortex B 5 pKi <10000 nM Ki J. Med. Chem. (1995) 38: 855-857 [PMID:7699699]
Histamine H1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3943] [UniProtKB: P31389]
ChEMBL The binding affinity (pKi) measured against histamine H1 receptor of guinea pig cerebellum using [3H]mepyramine as radioligand B 5 pKi <10000 nM Ki J. Med. Chem. (1995) 38: 855-857 [PMID:7699699]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 5.1 pIC50 7943.28 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL The binding affinity (pKi) was measured against 5-hydroxytryptamine 4 receptor of piglet hippocampus using [125I]-SB 207710 as radioligand B 5 pKi <10000 nM Ki J. Med. Chem. (1995) 38: 855-857 [PMID:7699699]
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
ChEMBL Antagonistic binding affinity measured against 5-hydroxytryptamine 2A receptor (human clone expressed in 293 cells) using [3H]ketanserin as radioligand B 5 pKi <10000 nM Ki J. Med. Chem. (1995) 38: 855-857 [PMID:7699699]
5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
ChEMBL The binding affinity (pKi) measured against 5-hydroxytryptamine 1E receptor (cloned human receptors in CHO cells) using [3H]5-HT1E as radioligand B 4 pKi <100000 nM Ki J. Med. Chem. (1995) 38: 855-857 [PMID:7699699]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Antagonistic binding affinity measured against 5-hydroxytryptamine 2C receptor (human clone expressed in 293 cells) using [3H]mesulergine as radioligand B 5.2 pKi <6309.57 nM Ki J. Med. Chem. (1995) 38: 855-857 [PMID:7699699]
ChEMBL Binding affinity analysed on 5-HT 2A human clone using [3H]ketanserin as radioligand B 5.2 pKi >6309.57 nM Ki J. Med. Chem. (1996) 39: 2773-2780 [PMID:8709108]
5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
GtoPdb - - 6.9 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL323] [GtoPdb: 7] [UniProtKB: P30994]
ChEMBL Antagonistic affinity measured as pA2 value on 5-hydroxytryptamine 2B receptor of the rat stomach fundus F 7.95 pKd 11.22 nM Kd J. Med. Chem. (1995) 38: 855-857 [PMID:7699699]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
GtoPdb - - 5.6 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]
ChEMBL The binding affinity (pKi) measured against 5-hydroxytryptamine 3 receptor of rat hippocampus and entorhinal cortex using [3H]granisetron as radioligand F 5.82 pKi 1513.56 nM Ki J. Med. Chem. (1995) 38: 855-857 [PMID:7699699]
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 5.82 pKi 1513.56 nM Ki J. Med. Chem. (1996) 39: 2773-2780 [PMID:8709108]
5-HT3A/5-HT3B/Serotonin 3 (5-HT3) receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094116] [GtoPdb: 373, 374] [UniProtKB: P35563, Q9JJ16]
ChEMBL The binding affinity (pKi) measured against 5-hydroxytryptamine 1A receptor of rat cortex using [3H]8-OH-DPAT as radioligand B 5 pKi <10000 nM Ki J. Med. Chem. (1995) 38: 855-857 [PMID:7699699]
5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639]
ChEMBL The binding affinity (pKi) was measured against 5-hydroxytryptamine 4 receptor of piglet hippocampus using [125I]SB 207710 as radioligand B 5 pKi <10000 nM Ki J. Med. Chem. (1995) 38: 855-857 [PMID:7699699]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]