SB 204070 [Ligand Id: 256] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL68131 (SB-204070) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944] | ||||||||
| ChEMBL | Tested against adrenergic alpha-1 receptor radiolabeled with [3H]7-methoxyprazosin | B | 6 | pKi | <1000 | nM | Ki | J Med Chem (1993) 36: 4121-4123 [PMID:8258837] |
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
| ChEMBL | Tested against adrenergic alpha-2 receptor | B | 6 | pKi | <1000 | nM | Ki | J Med Chem (1993) 36: 4121-4123 [PMID:8258837] |
| β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588] | ||||||||
| ChEMBL | Tested against Beta-1 adrenergic receptor | B | 6 | pKi | <1000 | nM | Ki | J Med Chem (1993) 36: 4121-4123 [PMID:8258837] |
| β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550] | ||||||||
| ChEMBL | Tested against Beta-2 adrenergic receptor | B | 6 | pKi | <1000 | nM | Ki | J Med Chem (1993) 36: 4121-4123 [PMID:8258837] |
| D1 receptor/Dopamine D1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3071] [GtoPdb: 214] [UniProtKB: Q61616] | ||||||||
| ChEMBL | Tested against dopamine receptor D1 | B | 6 | pKi | <1000 | nM | Ki | J Med Chem (1993) 36: 4121-4123 [PMID:8258837] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Tested against dopamine receptor D2 using cloned human receptor expressed in CHO cells radiolabeled with [125I]iodosulpiride | B | 5 | pKi | <10000 | nM | Ki | J Med Chem (1993) 36: 4121-4123 [PMID:8258837] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | Tested against dopamine receptor D3 using cloned human receptor expressed in CHO cells radiolabeled with [125I]iodosulpiride | B | 6 | pKi | <1000 | nM | Ki | J Med Chem (1993) 36: 4121-4123 [PMID:8258837] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3737] [GtoPdb: 1] [UniProtKB: Q64264] | ||||||||
| ChEMBL | Tested against 5-hydroxytryptamine 1A receptor | B | 6 | pKi | <1000 | nM | Ki | J Med Chem (1993) 36: 4121-4123 [PMID:8258837] |
| 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
| ChEMBL | Tested against 5-hydroxytryptamine 1D receptor | B | 5 | pKi | <10000 | nM | Ki | J Med Chem (1993) 36: 4121-4123 [PMID:8258837] |
| 5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566] | ||||||||
| ChEMBL | Tested for binding affinity towards cloned human 5-hydroxytryptamine 1E receptor using [3H]5-HT as radioligand | B | 5 | pKi | <10000 | nM | Ki | J Med Chem (1993) 36: 4121-4123 [PMID:8258837] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Tested against 5-hydroxytryptamine 2A receptor | B | 6 | pKi | <1000 | nM | Ki | J Med Chem (1993) 36: 4121-4123 [PMID:8258837] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Tested agains t5-hydroxytryptamine 2C receptor in experiment 1 | B | 6.9 | pKi | 125.89 | nM | Ki | J Med Chem (1993) 36: 4121-4123 [PMID:8258837] |
| ChEMBL | Tested against 5-hydroxytryptamine 2C receptor in experiment 2 | B | 7.1 | pKi | 79.43 | nM | Ki | J Med Chem (1993) 36: 4121-4123 [PMID:8258837] |
| 5-HT3E/5-HT3B/5-HT3A/5-HT3D/5-HT3C/Serotonin 3 (5-HT3) receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094132] [GtoPdb: 377, 374, 373, 376, 375] [UniProtKB: A5X5Y0, O95264, P46098, Q70Z44, Q8WXA8] | ||||||||
| ChEMBL | Tested against 5-hydroxytryptamine 3 receptor in experiment 1 | B | 6.6 | pKi | 251.19 | nM | Ki | J Med Chem (1993) 36: 4121-4123 [PMID:8258837] |
| ChEMBL | Tested against 5-hydroxytryptamine 3 receptor in experiment 2 | B | 6.7 | pKi | 199.53 | nM | Ki | J Med Chem (1993) 36: 4121-4123 [PMID:8258837] |
| 5-HT3A/Serotonin 3a (5-HT3a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098] | ||||||||
| ChEMBL | Binding affinity at 5HT3 receptor | B | 6.8 | pKi | 158.49 | nM | Ki | Bioorg Med Chem (2009) 17: 2607-2622 [PMID:19261477] |
| 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639] | ||||||||
| GtoPdb | - | - | 10.41 | pKi | 0.04 | nM | Ki |
J Neurochem (1997) 69: 1810-9 [PMID:9349523]; J Neurochem (2000) 74: 478-89 [PMID:10646498]; Br J Pharmacol (2000) 129: 771-81 [PMID:10683202]; Br J Pharmacol (2000) 131: 827-35 [PMID:11030734] |
| ChEMBL | Binding affinity at 5HT4 receptor | B | 10.8 | pKi | 0.02 | nM | Ki | Bioorg Med Chem (2009) 17: 2607-2622 [PMID:19261477] |
| Serotonin 4 (5-HT4) receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2696] [UniProtKB: Q6Q253] | ||||||||
| ChEMBL | Compound was evaluated for its ability to inhibit the binding of 5-HT4 receptor radioligand [125I]SB 207710 to piglet hippocampal membrane | B | 9.9 | pKi | 0.13 | nM | Ki | Bioorg Med Chem Lett (1994) 4: 667-668 |
| 5-HT4 receptor in Rat [GtoPdb: 9] [UniProtKB: Q62758] | ||||||||
| GtoPdb | - | - | 9.5 | pKi | - | - | - | Neuropharmacology (1997) 36: 671-9 [PMID:9225293] |
| Serotonin 4 (5-HT4) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5017] [UniProtKB: O70528] | ||||||||
| ChEMBL | Binding affinity to 5HT4 receptor in guinea pig distal colon | B | 10.7 | pKd | 0.02 | nM | Kd | Bioorg Med Chem Lett (2013) 23: 6243-6247 [PMID:24157369] |
| ChEMBL | Compound was tested for binding affinity against 5-HT4 receptor in guinea pig striata using [3H]GR-113808 as radioligand | B | 10.89 | pKi | 0.01 | nM | Ki | Bioorg Med Chem Lett (1994) 4: 2481-2484 |
| ChEMBL | Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP) | F | 10 | pIC50 | 0.1 | nM | IC50 | J Med Chem (1993) 36: 4121-4123 [PMID:8258837] |
| ChEMBL | Ability to block 5-HT4 receptor mediated effect of 5-HT was assessed in the guinea-pig distal colon longitudinal muscle myenteric plexus preparation (LMMP) | B | 10.1 | pIC50 | 0.08 | nM | IC50 | Bioorg Med Chem Lett (1994) 4: 667-668 |
| ChEMBL | Ability to antagonize 5-HT-evoked contractions mediated through 5-hydroxytryptamine 4 receptor activation in the guinea pig distal colon LMMP | B | 10.1 | pIC50 | 0.08 | nM | IC50 | J Med Chem (1995) 38: 4760-4763 [PMID:7490724] |
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]
