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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
