quipazine [Ligand Id: 173] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL18772 (Quipazine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588] | ||||||||
| ChEMBL | Binding affinity to His-tagged human beta1 adrenergic receptor expressed in HEK293 cell membranes by surface plasmon resonance analysis | B | 5.25 | pKd | 5623.41 | nM | Kd | J Med Chem (2013) 56: 3446-3455 [PMID:23517028] |
| ChEMBL | Binding affinity to His-tagged human beta1 adrenergic receptor expressed in HEK293 cell membranes by surface plasmon resonance analysis | B | 5.25 | pKd | 5600 | nM | Kd | J Med Chem (2013) 56: 3446-3455 [PMID:23517028] |
| ChEMBL | Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis | B | 5.2 | pKi | 6309.57 | nM | Ki | J Med Chem (2013) 56: 3446-3455 [PMID:23517028] |
| Neutrophil cytosol factor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1613743] [UniProtKB: P14598] | ||||||||
| ChEMBL | Binding affinity to immobilized recombinant human His-tagged p47phox SH3A-B domain (151 to 285 residues) expressed in Escherichia coli BL21 (DE3) cells assessed as dissociation constant by SPR assay | B | 3.38 | pKd | 420000 | nM | Kd | J Med Chem (2020) 63: 1156-1177 [PMID:31922756] |
| ChEMBL | Covalent inhibition of recombinant human His-tagged p47phox SH3A-B domain (151 to 285 residues) expressed in Escherichia coli BL21 (DE3) cells interaction with Cy5-p22phox149-162 incubated for 10 mins by fluorescence polarization competition assay | B | 2.85 | pKi | 1410000 | nM | Ki | J Med Chem (2020) 63: 1156-1177 [PMID:31922756] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Binding affinity to 5HT1A receptor | B | 5.7 | pKd | 1995.26 | nM | Kd | J Med Chem (2009) 52: 6107-6125 [PMID:19754201] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from 5HT1A receptor in cerebral cortex homogenates after 15 mins | B | 6.64 | pKi | 230 | nM | Ki | Eur J Med Chem (2012) 49: 200-210 [PMID:22309909] |
| ChEMBL | Binding affinity for 5-hydroxytryptamine 1A receptor | B | 5.84 | pIC50 | 1445.44 | nM | IC50 | J Med Chem (1996) 39: 2068-2080 [PMID:8642566] |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 1A receptor was measured using [3H]8-OH-DPAT as radioligand | B | 5.84 | pIC50 | 1445.44 | nM | IC50 | J Med Chem (1997) 40: 1808-1819 [PMID:9191957] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
| ChEMBL | Ability to displace [3H]- -OH-DPAT bound to 5-hydroxytryptamine 1A receptor in rat hippocampus | B | 5.44 | pKi | 3600 | nM | Ki | J Med Chem (1998) 41: 728-741 [PMID:9513601] |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 1A receptor of rat hippocampus tissue. | B | 5.44 | pKi | 3600 | nM | Ki | J Med Chem (1999) 42: 1556-1575 [PMID:10229626] |
| ChEMBL | Evaluated for the binding affinity to hippocampus striatal membranes at 5-hydroxytryptamine 1A receptor binding site by using [3H]-8-OH- DPAT as a radioligand. | B | 5.48 | pKi | 3300 | nM | Ki | J Med Chem (1987) 30: 1-12 [PMID:3543362] |
| ChEMBL | The compound was tested for the binding affinity against 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand. | B | 5.8 | pKi | 1584.89 | nM | Ki | J Med Chem (1999) 42: 4362-4379 [PMID:10543880] |
| ChEMBL | Displacement of [3H]8-OHDPAT from 5HT1A receptor in rat hippocampus | B | 5.8 | pKi | 1584 | nM | Ki | J Med Chem (2009) 52: 6946-6950 [PMID:19831400] |
| ChEMBL | Displacement of [3H]8-OHDPAT from 5HT1A receptor in rat hippocampus | B | 5.8 | pKi | 1584 | nM | Ki | J Med Chem (2009) 52: 3548-3562 [PMID:19425598] |
| ChEMBL | The compound was tested for their binding affinity towards 5-hydroxytryptamine 1A receptor from rat hippocampus using [3H]-8-OH-DPAT as radioligand | B | 5.82 | pKi | 1500 | nM | Ki | J Med Chem (1995) 38: 2692-2704 [PMID:7629808] |
| ChEMBL | Inhibition of radiolabeled [3H]-8-OH-DPAT ligand binding to 5-hydroxytryptamine 1A receptor | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (1997) 40: 3670-3678 [PMID:9357534] |
| 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564] | ||||||||
| ChEMBL | Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand. | B | 6.49 | pKi | 320 | nM | Ki | J Med Chem (1987) 30: 1-12 [PMID:3543362] |
| ChEMBL | Ability to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatum | B | 6.51 | pKi | 310 | nM | Ki | J Med Chem (1998) 41: 728-741 [PMID:9513601] |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatum. | B | 6.51 | pKi | 310 | nM | Ki | J Med Chem (1999) 42: 1556-1575 [PMID:10229626] |
| ChEMBL | The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand | B | 6.68 | pKi | 208 | nM | Ki | J Med Chem (1995) 38: 2692-2704 [PMID:7629808] |
| ChEMBL | The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand. | B | 6.7 | pKi | 199.53 | nM | Ki | J Med Chem (1999) 42: 4362-4379 [PMID:10543880] |
| ChEMBL | Binding affinity for 5-hydroxytryptamine 1B receptor | B | 5.15 | pIC50 | 7079.46 | nM | IC50 | J Med Chem (1996) 39: 2068-2080 [PMID:8642566] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand | B | 5.15 | pIC50 | 7079.46 | nM | IC50 | J Med Chem (1997) 40: 1808-1819 [PMID:9191957] |
| ChEMBL | Inhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptor | B | 6.42 | pIC50 | 380 | nM | IC50 | J Med Chem (1997) 40: 3670-3678 [PMID:9357534] |
| Serotonin 1d (5-HT1d) receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105] [UniProtKB: P79400] | ||||||||
| ChEMBL | Binding affinity for 5-hydroxytryptamine 1D receptor | B | 5.43 | pIC50 | 3715.35 | nM | IC50 | J Med Chem (1996) 39: 2068-2080 [PMID:8642566] |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 1D receptor was measured using [3H]5-HT as radioligand | B | 5.43 | pIC50 | 3715.35 | nM | IC50 | J Med Chem (1997) 40: 1808-1819 [PMID:9191957] |
| 5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| GtoPdb | - | - | 6.9 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733] |
| Serotonin 2a (5-HT2a) receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3446] [UniProtKB: Q75Z89] | ||||||||
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 2A receptor | B | 5.46 | pIC50 | 3467.37 | nM | IC50 | J Med Chem (1996) 39: 2068-2080 [PMID:8642566] |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 2A receptor was measured using [3H]ketanserin as radioligand | B | 5.46 | pIC50 | 3467.37 | nM | IC50 | J Med Chem (1997) 40: 1808-1819 [PMID:9191957] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842] | ||||||||
| ChEMBL | Ability to displace [3H]- ketanserin bound to 5-hydroxytryptamine 2A receptor in rat pre-frontal cortex | B | 5.74 | pKi | 1800 | nM | Ki | J Med Chem (1998) 41: 728-741 [PMID:9513601] |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 2A receptor of rat pre-frontal cortex. | B | 5.74 | pKi | 1800 | nM | Ki | J Med Chem (1999) 42: 1556-1575 [PMID:10229626] |
| ChEMBL | The compound was tested for the binding affinity against 5-hydroxytryptamine 2A receptor using [3H]ketanserin as radioligand. | B | 6.1 | pKi | 794.33 | nM | Ki | J Med Chem (1999) 42: 4362-4379 [PMID:10543880] |
| ChEMBL | Displacement of [3H]ketanserin from 5HT2A receptor in rat cortex | B | 6.1 | pKi | 794 | nM | Ki | J Med Chem (2009) 52: 3548-3562 [PMID:19425598] |
| ChEMBL | Displacement of [3H]ketanserin from 5HT2A receptor in rat cortex | B | 6.1 | pKi | 794 | nM | Ki | J Med Chem (2009) 52: 6946-6950 [PMID:19831400] |
| ChEMBL | Binding affinity to 5-hydroxytryptamine 2A receptor from rat cortex assayed using [3H]ketanserin as radioligand. | B | 6.89 | pKi | 130 | nM | Ki | J Med Chem (1995) 38: 2692-2704 [PMID:7629808] |
| ChEMBL | Inhibition of radiolabeled [3H]-Ketanserin ligand binding to 5-hydroxytryptamine 2A receptor | B | 5.85 | pIC50 | 1400 | nM | IC50 | J Med Chem (1997) 40: 3670-3678 [PMID:9357534] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Evaluated for the binding affinity to porcine choroid plexus at 5-hydroxytryptamine 2C receptor binding site by using [3H]-MES as a radioligand. | B | 6.7 | pKi | 200 | nM | Ki | J Med Chem (1987) 30: 1-12 [PMID:3543362] |
| GtoPdb | - | - | 7.3 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]; J Neurochem (1999) 72: 2127-34 [PMID:10217294]; Synapse (2000) 35: 144-50 [PMID:10611640] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 2C receptor | B | 7.21 | pIC50 | 61.66 | nM | IC50 | J Med Chem (1996) 39: 2068-2080 [PMID:8642566] |
| ChEMBL | Binding affinity against 5-Hydroxytryptamine 2C Receptor was measured using [3H]N-methyl-mesulergine as radioligand | B | 7.21 | pIC50 | 61.66 | nM | IC50 | J Med Chem (1997) 40: 1808-1819 [PMID:9191957] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909] | ||||||||
| ChEMBL | The compound was tested for the binding affinity against 5-hydroxytryptamine 2C receptor using [3H]Mesulergine as radioligand. | B | 6.5 | pKi | 316.23 | nM | Ki | J Med Chem (1999) 42: 4362-4379 [PMID:10543880] |
| ChEMBL | Ability to displace [3H]mesulergine bound to 5-hydroxytryptamine 2C receptor in rat cortex | B | 6.72 | pKi | 190 | nM | Ki | J Med Chem (1998) 41: 728-741 [PMID:9513601] |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 2C receptor of rat cortex. | B | 6.72 | pKi | 190 | nM | Ki | J Med Chem (1999) 42: 1556-1575 [PMID:10229626] |
| ChEMBL | Inhibition of radiolabeled [3H]mesulergine ligand binding to 5-hydroxytryptamine 2C receptor | B | 6.33 | pIC50 | 470 | nM | IC50 | J Med Chem (1997) 40: 3670-3678 [PMID:9357534] |
| 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 | Compound was tested for the inhibition of [3H]GR-65630 binding to 5-hydroxytryptamine 3 receptor expressed in NG 108-15 cells | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (1996) 39: 4017-4026 [PMID:8831767] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 3 receptor | B | 8.74 | pKi | 1.8 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 2743-2747 [PMID:12217367] |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 3 receptor was measured using [3H]granisetron as radioligand | B | 9.35 | pIC50 | 0.45 | nM | IC50 | J Med Chem (1997) 40: 1808-1819 [PMID:9191957] |
| ChEMBL | Effective concentration against 5-Hydroxytryptamine 3 receptor by measuring [14C]guanidinium uptake on NG108-15 cells. | F | 9 | pEC50 | 1 | nM | EC50 | J Med Chem (1999) 42: 4362-4379 [PMID:10543880] |
| 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 compound was tested for the binding affinity against 5-hydroxytryptamine 3 receptor using [3H]zacopride as radioligand. | B | 8.2 | pKi | 6.31 | nM | Ki | J Med Chem (1999) 42: 4362-4379 [PMID:10543880] |
| ChEMBL | Inhibitory activity against 5-hydroxytryptamine 3 receptor in rat cortical membranes using [3H]- 1-Methyl-1H-indazole-3-carboxylic acid (8-methyl-8-aza-bicyclo[3.2.1]oct-3-yl)-amide as a radioligand | B | 8.52 | pKi | 3.04 | nM | Ki | J Med Chem (1990) 33: 3176-3181 [PMID:2258903] |
| ChEMBL | pKi value for inhibition of [3H]LY-278584 binding to 5-hydroxytryptamine 3 receptor | B | 8.52 | pKi | 3.02 | nM | Ki | J Med Chem (1990) 33: 3176-3181 [PMID:2258903] |
| ChEMBL | Binding affinity at 5-hydroxytryptamine 3 receptor in rat cortical membrane by [3H]graniestron displacement. | B | 8.74 | pKi | 1.82 | nM | Ki | J Med Chem (1998) 41: 728-741 [PMID:9513601] |
| ChEMBL | Inhibition of [3H]granisetron binding to 5-hydroxytryptamine 3 receptor of rat cortical membrane | B | 8.74 | pKi | 1.8 | nM | Ki | J Med Chem (1999) 42: 1556-1575 [PMID:10229626] |
| ChEMBL | Ability to displace [3H]granisetron specifically bound to 5-hydroxytryptamine 3 receptor in rat cortical membrane | B | 8.74 | pKi | 1.8 | nM | Ki | J Med Chem (1998) 41: 728-741 [PMID:9513601] |
| ChEMBL | Binding affinity to 5-hydroxytryptamine 3 receptor using [3H]GR-65630 as radioligand in rat cortex | B | 8.85 | pKi | 1.41 | nM | Ki | J Med Chem (1990) 33: 1594-1600 [PMID:2342053] |
| ChEMBL | Compound was evaluated for its binding affinity for 5-hydroxytryptamine 3 receptor by measuring displacement [3H]GR-65630 in rat cerebral cortex | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (1998) 41: 311-317 [PMID:9464362] |
| ChEMBL | Binding affinity for 5-hydroxytryptamine 3 receptor from rat cortex using [3H]BRL-43694 as radioligand | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (1995) 38: 2692-2704 [PMID:7629808] |
| ChEMBL | Binding affinity to 5-hydroxytryptamine 3 receptor using [3H]quipazine as radioligand in rat cortex | B | 9 | pKi | 1 | nM | Ki | J Med Chem (1990) 33: 1594-1600 [PMID:2342053] |
| ChEMBL | Inhibition of [3H]BRL-43694 binding to 5-hydroxytryptamine 3 receptor of rat cortical homogenate. | B | 8.21 | pIC50 | 6.2 | nM | IC50 | J Med Chem (1997) 40: 3670-3678 [PMID:9357534] |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 3 (5-HT3) receptor from rat cortical homogenate using [3H]zacopride as radioligand | B | 8.42 | pIC50 | 3.8 | nM | IC50 | J Med Chem (1999) 42: 4362-4379 [PMID:10543880] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 3 receptor | B | 9.35 | pIC50 | 0.45 | nM | IC50 | J Med Chem (1996) 39: 2068-2080 [PMID:8642566] |
| 5-HT3A/Serotonin 3a (5-HT3a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098] | ||||||||
| ChEMBL | Displacement of [3H]GR65630 from human 5HT3A receptor in HEK293 cells | B | 8.4 | pKi | 3.98 | nM | Ki | J Med Chem (2007) 50: 4616-4629 [PMID:17722904] |
| ChEMBL | Displacement of [3H]GR65630 from human 5HT3A receptor in HEK293 cells | B | 8.43 | pKi | 3.7 | nM | Ki | J Med Chem (2007) 50: 4616-4629 [PMID:17722904] |
| 5-HT3A/Serotonin 3a (5-HT3a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2411] [GtoPdb: 373] [UniProtKB: P35563] | ||||||||
| ChEMBL | Displacement of [3H]LY278584 from 5HT3 receptor in rat cortical homogenate | B | 9.02 | pKi | 0.96 | nM | Ki | J Med Chem (2009) 52: 3548-3562 [PMID:19425598] |
| ChEMBL | Displacement of [3H]LY278584 from 5HT3 receptor in rat cortical homogenate | B | 9.02 | pKi | 0.96 | nM | Ki | J Med Chem (2009) 52: 6946-6950 [PMID:19831400] |
| 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758] | ||||||||
| ChEMBL | Inhibition of radiolabeled [3H]GR-113808 ligand binding to 5-hydroxytryptamine 4 receptor | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (1997) 40: 3670-3678 [PMID:9357534] |
| Serotonin 4 (5-HT4) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5017] [UniProtKB: O70528] | ||||||||
| ChEMBL | The compound was tested for the binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand. | B | 5 | pKi | <10000 | nM | Ki | J Med Chem (1999) 42: 4362-4379 [PMID:10543880] |
| ChEMBL | Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2009) 52: 3548-3562 [PMID:19425598] |
| ChEMBL | Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2009) 52: 6946-6950 [PMID:19831400] |
| 5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3597] [GtoPdb: 10] [UniProtKB: P30966] | ||||||||
| ChEMBL | Binding affinity towards murine 5-hydroxytryptamine 5A receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| ChEMBL | Binding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]LSD as radioligand | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
| ChEMBL | Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand | B | 5.44 | pKi | 3600 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
| ChEMBL | Binding affinity of compound towards rodent 5-hydroxytryptamine 7 receptor | B | 5.52 | pKi | 3033 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
| ChEMBL | Displacement of [3H]-5HT from human SERT | B | 7.52 | pKi | 30 | nM | Ki | Eur J Med Chem (2012) 49: 200-210 [PMID:22309909] |
| SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] | ||||||||
| ChEMBL | Inhibition of [3H]citalopram binding to Serotonin transporter of rat cerebral cortex | B | 7.2 | pKi | 63 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1559-1562 [PMID:10915050] |
| ChEMBL | Effect of compound on Serotonin transporter uptake from rat cortex using [3H]citalopram as radioligand | B | 7.37 | pKi | 43 | nM | Ki | J Med Chem (1995) 38: 2692-2704 [PMID:7629808] |
| ChEMBL | Ability to displace [3H]paroxetine bound to Serotonin transporter receptor in rat forebrain | B | 7.51 | pKi | 31 | nM | Ki | J Med Chem (1998) 41: 728-741 [PMID:9513601] |
| ChEMBL | Binding affinity towards Serotonin transporter was determined in rat forebrain membrane | B | 7.51 | pKi | 31 | nM | Ki | J Med Chem (1999) 42: 1556-1575 [PMID:10229626] |
| 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| GtoPdb | - | - | 7.1 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733] |
| 5-HT2B receptor in Rat [GtoPdb: 7] [UniProtKB: P30994] | ||||||||
| GtoPdb | - | - | 6.9 | pKi | - | - | - | Mol Pharmacol (1993) 43: 419-26 [PMID:8450835] |
| 5-HT3AB in Human [GtoPdb: 378] | ||||||||
| GtoPdb | - | - | 9 | pKi | - | - | - | Neuropharmacology (2001) 41: 282-4 [PMID:11489465] |
| 5-HT3A in Human [GtoPdb: 379] | ||||||||
| GtoPdb | - | - | 9.5 | pKi | - | - | - | Neuropharmacology (2001) 41: 282-4 [PMID:11489465] |
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]
