duloxetine [Ligand Id: 202] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL1175 (Cymbalta, Duloxetine, LY-248686, LY248686) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959] | ||||||||
| ChEMBL | Displacement of [3H]WIN35428 from human DAT transfected in HEK293 cells after 3 hrs by Wallac counting analysis | B | 6.32 | pKi | 484 | nM | Ki | ACS Med Chem Lett (2013) 4: 560-564 [PMID:24900709] |
| ChEMBL | Displacement of [3H]dopamine from human DAT expressed in HEK293 cells by scintillation proximity assay | B | 6.36 | pKi | 435 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 3788-3792 [PMID:20471260] |
| ChEMBL | Inhibition of [3H]dopamine reuptake at human DAT expressed in HEK293 cells | B | 6.36 | pKi | 435 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 2562-2566 [PMID:18387300] |
| ChEMBL | Displacement of [3H]dopamine from human DAT receptor expressed in HEK293 cells by scintillation counting | B | 6.36 | pKi | 435 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 5078-5081 [PMID:19647430] |
| ChEMBL | Inhibition constant against dopamine transporter | B | 6.43 | pKi | 370 | nM | Ki | J Med Chem (2005) 48: 6523-6543 [PMID:16220969] |
| ChEMBL | Displacement of [3H]WIN35428 from human recombinant DAT transfected in HEK293 cell membrane | B | 6.5 | pKi | 316.23 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 1456-1461 [PMID:23347683] |
| ChEMBL | Inhibition of DAT | B | 6.6 | pKi | 251.19 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 4630-4633 [PMID:19592243] |
| ChEMBL | Ability to inhibit the reuptake of dopamine at human dopamine transporter | B | 6.62 | pKi | 240 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 4477-4480 [PMID:14643350] |
| ChEMBL | Ability to inhibit [3H]WIN-35428 binding to cloned human dopamine (DA) transporter | B | 6.62 | pKi | 240 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 3481-3486 [PMID:15177457] |
| ChEMBL | Displacement of [3H]WIN-35428 form human DAT expressed in CHO cell membranes | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 2809-2812 [PMID:20378347] |
| ChEMBL | Inhibition of human DAT expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay | B | 6.01 | pIC50 | 977 | nM | IC50 | ACS Med Chem Lett (2014) 5: 999-1004 [PMID:25221656] |
| ChEMBL | Inhibition of DA reuptake at human DAT expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay | B | 6.01 | pIC50 | 977 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 3234-3237 [PMID:24974340] |
| ChEMBL | Inhibition of [3H]DA reuptake at DA transporter in HEK293 cells | B | 6.06 | pIC50 | 870 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 4349-4353 [PMID:16750363] |
| ChEMBL | Inhibition of DA transporter expressed in HEK293 cells | B | 6.06 | pIC50 | 870 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 4345-4348 [PMID:16750359] |
| ChEMBL | Inhibition of [3H]DA from human DAT expressed in HEK293 cells | B | 6.06 | pIC50 | 870 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 2022-2025 [PMID:17267217] |
| ChEMBL | Displacement of 3,4-[ring-2,5,6-3H]dihydroxyphenylethylamine from human cloned DAT expressed in HEK293 cells by microplate scintillation counter | B | 6.18 | pIC50 | 660 | nM | IC50 | J Med Chem (2008) 51: 7265-7272 [PMID:18954038] |
| ChEMBL | Inhibition of human DAT | B | 6.18 | pIC50 | 660 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 1346-1349 [PMID:18207394] |
| ChEMBL | Inhibition of [3H]DA uptake at human DAT expressed in HEK293 cells | B | 6.23 | pIC50 | 590 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2829-2834 [PMID:19359175] |
| DAT/Dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977] | ||||||||
| ChEMBL | Displacement of [125I]RTI55 from DAT in Sprague-dawley rat striatum by liquid scintillation spectrophotometry | B | 6.43 | pIC50 | 370 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 58-61 [PMID:19038547] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) K1 cells stably expressing hERG measured using IonWorks Quattro automated patch clamp platform | F | 5 | pIC50 | 10000 | nM | IC50 | J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753] |
| ChEMBL | Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) cells stable expressing hERG measured using IonWorks Barracuda automated patch clamp platform | F | 5.2 | pIC50 | 6309.57 | nM | IC50 | J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753] |
| ChEMBL | Inhibition of rapid delayed inward rectifying potassium current (IKr) measured using manual patch clamp assay | F | 5.3 | pIC50 | 5011.87 | nM | IC50 | J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753] |
| H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1] | ||||||||
| ChEMBL | Displacement of [3H]N-R-methylhistamine from human H3 receptor isolated from C6 cells | B | 5.3 | pKi | >5000 | nM | Ki | J Med Chem (2010) 53: 7869-7873 [PMID:20945906] |
| H3 receptor/Histamine H3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8] | ||||||||
| ChEMBL | Displacement of [3H]N-R-methylhistamine from rat H3 receptor | B | 5.3 | pKi | >5000 | nM | Ki | J Med Chem (2010) 53: 7869-7873 [PMID:20945906] |
| NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] | ||||||||
| ChEMBL | Displacement of [3H]noradrenaline from human NET receptor expressed in HEK293 cells by scintillation counting | B | 7.35 | pKi | 45 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 5078-5081 [PMID:19647430] |
| ChEMBL | Displacement of [3H]nisoxetine from human NET expressed in HEK293 cells by scintillation proximity assay | B | 7.35 | pKi | 45 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 3788-3792 [PMID:20471260] |
| ChEMBL | Inhibition of [3H]nisoxetine reuptake at human NET expressed in HEK293 cells | B | 7.35 | pKi | 45 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 2562-2566 [PMID:18387300] |
| ChEMBL | Inhibition constant against norepinephrine transporter | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2005) 48: 6523-6543 [PMID:16220969] |
| ChEMBL | Inhibition of NET | B | 8.1 | pKi | 7.94 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 4630-4633 [PMID:19592243] |
| ChEMBL | Ability to inhibit the reuptake of NE at human norepinephrine transporter | B | 8.12 | pKi | 7.5 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 4477-4480 [PMID:14643350] |
| ChEMBL | Ability to inhibit [3H]nisoxetine binding to cloned human norepinephrine (NE) transporter | B | 8.13 | pKi | 7.45 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 3481-3486 [PMID:15177457] |
| ChEMBL | Displacement of [3H]Nisoxetine from human NET transfected in HEK293 cells after 3 hrs by Wallac counting analysis | B | 8.17 | pKi | 6.7 | nM | Ki | ACS Med Chem Lett (2013) 4: 560-564 [PMID:24900709] |
| GtoPdb | - | - | 8.22 | pKi | 5.97 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 7219-22 [PMID:23084899] |
| ChEMBL | Inhibition of human NET | B | 8.22 | pKi | 5.97 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 7219-7222 [PMID:23084899] |
| ChEMBL | Binding affinity to NET (unknown origin) | B | 8.34 | pKi | 4.6 | nM | Ki | J Med Chem (2021) 64: 10581-10605 [PMID:34313432] |
| ChEMBL | Inhibition of human NET expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay | B | 6.29 | pIC50 | 515 | nM | IC50 | ACS Med Chem Lett (2014) 5: 999-1004 [PMID:25221656] |
| ChEMBL | Inhibition of norepinephrine reuptake at human NET expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay | B | 6.29 | pIC50 | 515 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 3234-3237 [PMID:24974340] |
| ChEMBL | Displacement of [3H]Nisoxetine from human NET transfected in HEK293 cells after 3 hrs by Wallac counting analysis | B | 7.54 | pIC50 | 29 | nM | IC50 | ACS Med Chem Lett (2013) 4: 560-564 [PMID:24900709] |
| ChEMBL | Inhibition of [3H]NA reuptake at NA transporter in HEK293 cells | B | 7.72 | pIC50 | 19 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 4349-4353 [PMID:16750363] |
| ChEMBL | Inhibition of [3H]NA uptake at NA transporter expressed in HEK293 cells | B | 7.72 | pIC50 | 19 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 4345-4348 [PMID:16750359] |
| ChEMBL | Inhibition of [3H]NA from human NET expressed in HEK293 cells | B | 7.72 | pIC50 | 19 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 2022-2025 [PMID:17267217] |
| ChEMBL | Inhibition of human NET | B | 8.05 | pIC50 | 8.9 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 1346-1349 [PMID:18207394] |
| ChEMBL | Displacement of Levo[ring-2,5,6-3H]norepinephrine from human cloned NET expressed in HEK293 cells by microplate scintillation counter | B | 8.05 | pIC50 | 8.9 | nM | IC50 | J Med Chem (2008) 51: 7265-7272 [PMID:18954038] |
| ChEMBL | Inhibition of [3H]NA uptake at human NET expressed in HEK293 cells | B | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2829-2834 [PMID:19359175] |
| ChEMBL | Inhibition of human NET transfected in MDCK-Net6 cells | B | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 2809-2812 [PMID:20378347] |
| ChEMBL | Inhibition of norepinephrine uptake at human NET expressed in MDCK-Net6 cells | B | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2464-2467 [PMID:19329313] |
| ChEMBL | Inhibition of norepinephrine uptake at human NET expressed in MDCK cells | B | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 4929-4931 [PMID:18771916] |
| ChEMBL | Inhibition of human recombinant NET expressed in HEK293 cells assessed as inhibition of [3H]NE reuptake | B | 8.8 | pIC50 | 1.58 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 1456-1461 [PMID:23347683] |
| Serine hydroxymethyltransferase, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295747] [UniProtKB: P34897] | ||||||||
| ChEMBL | Inhibition of His-tagged human recombinant SHMT2 expressed in Escherichia coli BLR(DE3) assessed as reduction in NADPH level using L-serine, THF and NADP+ incubated for 5 mins by SHMT2-MTHFD coupled reaction based fluorescence assay | B | 5.16 | pIC50 | 6918.31 | nM | IC50 | WO-2016085990-A1. Compositions and methods relating to inhibiting serine hyrdoxymethyltransferase 2 activity (2016) |
| SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
| GtoPdb | - | - | 8.3 | pKi | 5 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 2562-6 [PMID:18387300] |
| ChEMBL | Displacement of [3H]citalopram from human SERT expressed in HEK293 cells by scintillation proximity assay | B | 8.3 | pKi | 5 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 3788-3792 [PMID:20471260] |
| ChEMBL | Inhibition of [3H]citalopram uptake at human 5HTT expressed in HEK293 cells | B | 8.3 | pKi | 5 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 2562-2566 [PMID:18387300] |
| ChEMBL | Displacement of [3H]5HT from human 5HT transporter expressed in HEK293 cells by scintillation counting | B | 8.3 | pKi | 5 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 5078-5081 [PMID:19647430] |
| ChEMBL | Inhibition constant against serotonin transporter | B | 8.34 | pKi | 4.6 | nM | Ki | J Med Chem (2005) 48: 6523-6543 [PMID:16220969] |
| ChEMBL | Ability to inhibit the reuptake of 5-HT at human serotonin transporter | B | 9.1 | pKi | 0.8 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 4477-4480 [PMID:14643350] |
| ChEMBL | Ability to inhibit [3H]paroxetine binding to cloned human serotonin (5-HT) transporter | B | 9.1 | pKi | 0.79 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 3481-3486 [PMID:15177457] |
| ChEMBL | Inhibition of SERT | B | 9.3 | pKi | 0.5 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 4630-4633 [PMID:19592243] |
| ChEMBL | Displacement of [3H]citalopram from human SERT transfected in HEK293 cells after 3 hrs by Wallac counting analysis | B | 9.62 | pKi | 0.24 | nM | Ki | ACS Med Chem Lett (2013) 4: 560-564 [PMID:24900709] |
| ChEMBL | Inhibition of human SERT expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay | B | 7.98 | pIC50 | 10.4 | nM | IC50 | ACS Med Chem Lett (2014) 5: 999-1004 [PMID:25221656] |
| ChEMBL | Inhibition of serotonin reuptake at human SERT expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay | B | 7.98 | pIC50 | 10.4 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 3234-3237 [PMID:24974340] |
| ChEMBL | Displacement of [alpha,beta-3H(N)]-5-hydroxytryptamine from human cloned SERT expressed in HEK293 cells by microplate scintillation counter | B | 8.18 | pIC50 | 6.6 | nM | IC50 | J Med Chem (2008) 51: 7265-7272 [PMID:18954038] |
| ChEMBL | Inhibition of human SERT | B | 8.18 | pIC50 | 6.6 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 1346-1349 [PMID:18207394] |
| ChEMBL | Inhibition of [3H]5-HT reuptake at 5HT transporter in HEK293 cells | B | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 4349-4353 [PMID:16750363] |
| ChEMBL | Inhibition of [3H]5-HT uptake at 5HT transporter expressed in HEK293 cells | B | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 4345-4348 [PMID:16750359] |
| ChEMBL | Inhibition of [3H]5-HT from human SERT expressed in HEK293 cells | B | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 2022-2025 [PMID:17267217] |
| ChEMBL | Inhibition of [3H]5-HT uptake at human 5HTT expressed in HEK293 cells | B | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2829-2834 [PMID:19359175] |
| ChEMBL | Inhibition of human SERT expressed in human JAR cells | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 2809-2812 [PMID:20378347] |
| ChEMBL | Inhibition of serotonin uptake at human SERT expressed in human JAR cells | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2464-2467 [PMID:19329313] |
| ChEMBL | Inhibition of serotonin uptake at human SERT expressed in JAR cells | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 4929-4931 [PMID:18771916] |
| ChEMBL | Displacement of [3H]citalopram from human SERT transfected in HEK293 cells after 3 hrs by Wallac counting analysis | B | 8.64 | pIC50 | 2.3 | nM | IC50 | ACS Med Chem Lett (2013) 4: 560-564 [PMID:24900709] |
| ChEMBL | Inhibition of human recombinant SERT expressed in HEK293 cells assessed as inhibition of [3H]5HT reuptake | B | 9.5 | pIC50 | 0.32 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 1456-1461 [PMID:23347683] |
| SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] | ||||||||
| ChEMBL | Displacement of [3H]citalopram from SERT in Sprague-dawley rat frontal cortex by liquid scintillation spectrophotometry | B | 8.34 | pKi | 4.6 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 58-61 [PMID:19038547] |
| ChEMBL | Displacement of [3H]-citalopram from Sprague-Dawley rat brain SERT after 1 hr | B | 10.09 | pKi | 0.08 | nM | Ki | ACS Med Chem Lett (2013) 4: 560-564 [PMID:24900709] |
| Nav1.5/Sodium channel protein type V alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524] | ||||||||
| ChEMBL | Inhibition of fast sodium current (INa) in HEK293 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform | F | 4.8 | pIC50 | 15848.93 | nM | IC50 | J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753] |
| ChEMBL | Inhibition of fast sodium current (INa) in Chinese Hamster Ovary (CHO) K1 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform | F | 5.1 | pIC50 | 7943.28 | nM | IC50 | J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753] |
| Transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6184] [UniProtKB: Q63380] | ||||||||
| ChEMBL | Displacement of [3H]nisoxetine from Sprague-dawley rat NET by liquid scintillation spectrophotometry | B | 7.8 | pKi | 16 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 58-61 [PMID:19038547] |
| ChEMBL | Inhibition of rat NET | B | 8.41 | pKi | 3.9 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 7219-7222 [PMID:23084899] |
| ChEMBL | Displacement of [3H]nisoxetine from rat NET in rat cerebral cortex | B | 8.52 | pKi | 3 | nM | Ki | J Med Chem (2010) 53: 7869-7873 [PMID:20945906] |
| Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936] | ||||||||
| ChEMBL | Inhibition of long-lasting type calcium current (hICa) in Chinese Hamster Ovary (CHO) cells expressing hCav1.2 measured using IonWorks Quattro automated patch clamp platform | F | 4 | pIC50 | 100000 | nM | IC50 | J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753] |
| ChEMBL | Inhibition of long-lasting type calcium current (ICaL) in HEK293 cells (alpha1C/beta2a/alpha2delta1) cells measured using IonWorks Barracuda automated patch clamp platform | F | 4.6 | pIC50 | 25118.86 | nM | IC50 | J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753] |
| Kv7.1/Voltage-gated potassium channel, IKs; KCNQ1(Kv7.1)/KCNE1(MinK) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2221347] [GtoPdb: 560] [UniProtKB: P15382, P51787] | ||||||||
| ChEMBL | Inhibition of slow delayed inward rectifying potassium current (Iks) in Chinese Hamster Ovary (CHO) cells expressing hKvLQT1/hminK measured using IonWorks Quattro automated patch clamp platform | F | 5 | pIC50 | 10000 | nM | IC50 | J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753] |
| Kv4.3/Voltage-gated potassium channel subunit Kv4.3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1964] [GtoPdb: 554] [UniProtKB: Q9UK17] | ||||||||
| ChEMBL | Inhibition of transient outward potassium current (Ito) current in Chinese Hamster Ovary (CHO) K1 cells expressing human Kv4.3 measured using IonWorks Quattro automated patch clamp platform | F | 4 | pIC50 | 100000 | nM | IC50 | J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753] |
| 5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| GtoPdb | - | - | 6.3 | pKi | - | - | - | Neuropsychopharmacology (2001) 25: 871-80 [PMID:11750180] |
| 5-HT2C receptor in Human [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| GtoPdb | - | - | 6 | pKi | - | - | - | Neuropsychopharmacology (2001) 25: 871-80 [PMID:11750180] |
| 5-HT6 receptor in Human [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
| GtoPdb | - | - | 6.4 | pKi | - | - | - | Neuropsychopharmacology (2001) 25: 871-80 [PMID:11750180] |
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]
