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: CHEMBL1323 ((-)-darunavir, Darunavir, MC-114, Prezista, TMC 114, TMC-114, TMC114, TMC-41629, UIC-94017, UIC-940T) |
---|
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 |
---|---|---|---|---|---|---|---|---|
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) cells stable expressing hERG measured using IonWorks Barracuda automated patch clamp platform | F | 4 | pIC50 | 100000 | 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) K1 cells stably expressing hERG measured using IonWorks Quattro automated patch clamp platform | F | 4.2 | pIC50 | 63095.73 | nM | IC50 | J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753] |
Human immunodeficiency virus type 1 protease in Human immunodeficiency virus 1 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL243] [UniProtKB: Q72874] | ||||||||
ChEMBL | Inhibition of HIV1 protease V32I mutant by competitive binding | B | 6.52 | pKi | 300 | nM | Ki | J Med Chem (2008) 51: 6599-6603 [PMID:18808097] |
ChEMBL | Inhibition of HIV1 protease V32I mutant by uncompetitive binding | B | 6.74 | pKi | 180 | nM | Ki | J Med Chem (2008) 51: 6599-6603 [PMID:18808097] |
ChEMBL | Inhibition of HIV1 protease V32I mutant by enzyme inhibition | B | 7.27 | pKi | 54 | nM | Ki | J Med Chem (2008) 51: 6599-6603 [PMID:18808097] |
ChEMBL | Binding affinity to HIV1 protease D30N | B | 8.18 | pKi | 6.6 | nM | Ki | J Med Chem (2006) 49: 1379-1387 [PMID:16480273] |
ChEMBL | Inhibitory activity against HIV-1 protease | B | 8.68 | pKi | 2.1 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 687-690 [PMID:9871583] |
ChEMBL | Binding affinity to HIV1 protease I50V | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2006) 49: 1379-1387 [PMID:16480273] |
ChEMBL | Inhibition of HIV1 protease D30N mutant | B | 8.72 | pKi | 1.9 | nM | Ki | J Med Chem (2007) 50: 4509-4515 [PMID:17696515] |
ChEMBL | Inhibition of HIV1 protease I50V mutant | B | 8.89 | pKi | 1.3 | nM | Ki | J Med Chem (2007) 50: 4509-4515 [PMID:17696515] |
ChEMBL | Binding affinity to HIV1 protease I84V | B | 8.96 | pKi | 1.1 | nM | Ki | J Med Chem (2006) 49: 1379-1387 [PMID:16480273] |
ChEMBL | Binding affinity to HIV1 protease V82A | B | 9.1 | pKi | 0.8 | nM | Ki | J Med Chem (2006) 49: 1379-1387 [PMID:16480273] |
ChEMBL | Inhibition of HIV1 protease I84V mutant | B | 9.25 | pKi | 0.56 | nM | Ki | J Med Chem (2007) 50: 4509-4515 [PMID:17696515] |
ChEMBL | Inhibition of HIV1 protease V82A mutant | B | 9.27 | pKi | 0.54 | nM | Ki | J Med Chem (2007) 50: 4509-4515 [PMID:17696515] |
ChEMBL | Inhibition of wild type HIV1 protease expressed in Escherichia coli using Arg-Glu (EDANS)-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-Lys(DABCYL)-Arg as substrate preincubated for 20 to 30 mins followed by substrate addition and measured for 10 mins by FRET assay | B | 9.47 | pKi | 0.34 | nM | Ki | ACS Med Chem Lett (2020) 11: 1196-1204 [PMID:32551001] |
ChEMBL | Inhibition of HIV1 recombinant protease V32I/I47A mutant expressed in Escherichia coli by spectrophotometric assay | B | 9.51 | pKi | 0.31 | nM | Ki | J Med Chem (2008) 51: 4839-4843 [PMID:18598016] |
ChEMBL | Binding affinity to HIV1 protease | B | 9.66 | pKi | 0.22 | nM | Ki | J Med Chem (2006) 49: 1379-1387 [PMID:16480273] |
ChEMBL | Inhibition of wild type HIV1 protease using Arg-Glu (EDANS)-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-Lys(DABCYL)-Arg as substrate preincubated for 20 to 30 mins followed by substrate addition and measured for 10 mins by FRET assay | B | 9.74 | pKi | 0.18 | nM | Ki | Eur J Med Chem (2021) 220: 113450-113450 [PMID:33906049] |
ChEMBL | Inhibition of HIV1 recombinant protease M46I/A71V/V82T/I84V mutant expressed in Escherichia coli by spectrophotometric assay | B | 10.49 | pKi | 0.03 | nM | Ki | J Med Chem (2008) 51: 4839-4843 [PMID:18598016] |
ChEMBL | Binding affinity to HIV1 protease L90M | B | 10.52 | pKi | 0.03 | nM | Ki | J Med Chem (2006) 49: 1379-1387 [PMID:16480273] |
ChEMBL | Inhibition of HIV1 protease L10I, L63P, A71V, G73S, I84V, L90M mutant by FRET assay | B | 10.57 | pKi | 0.03 | nM | Ki | J Med Chem (2012) 55: 6328-6341 [PMID:22708897] |
ChEMBL | Inhibition of HIV1 recombinant protease L10I/L24I/L33F/M46L/154V/L63P/A71V/V82A/I84V mutant expressed in Escherichia coli by spectrophotometric assay | B | 10.7 | pKi | 0.02 | nM | Ki | J Med Chem (2008) 51: 4839-4843 [PMID:18598016] |
ChEMBL | Inhibition of HIV1 recombinant protease L10I/I15V/E35D/N37S/R41K/I62V/L63P/A71V/G73S/L90M mutant expressed in Escherichia coli by spectrophotometric assay | B | 10.82 | pKi | 0.01 | nM | Ki | J Med Chem (2008) 51: 4839-4843 [PMID:18598016] |
ChEMBL | Inhibitory activity against human immunodeficiency virus 1 protease | B | 10.82 | pKi | 0.01 | nM | Ki | J Med Chem (2005) 48: 3576-3585 [PMID:15887965] |
ChEMBL | Inhibition of HIV1 protease | B | 10.85 | pKi | 0.01 | nM | Ki | J Med Chem (2006) 49: 5252-5261 [PMID:16913714] |
ChEMBL | Inhibition of HIV1 recombinant protease D30N/N88D mutant expressed in Escherichia coli by spectrophotometric assay | B | 10.96 | pKi | 0.01 | nM | Ki | J Med Chem (2008) 51: 4839-4843 [PMID:18598016] |
ChEMBL | Inhibition of HIV1 protease by FRET assay | B | 6.43 | pIC50 | 370 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127019-127019 [PMID:32057582] |
ChEMBL | Inhibition of HIV-1 protease expressed in Escherichia coli using Arg-Glu(EDANS)-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-Lys(DABCYL)-Arg as substrate preincubated for 20 to 30 mins followed by substrate addition by FRET based assay | B | 8.53 | pIC50 | 2.92 | nM | IC50 | Bioorg Med Chem (2020) 28: 115623-115623 [PMID:32690263] |
ChEMBL | Inhibition of recombinant HIV1 protease measured assessed as hydrolysis of fluorogenic substrate by FRET assay | B | 8.76 | pIC50 | 1.72 | nM | IC50 | Eur J Med Chem (2020) 186: 111900-111900 [PMID:31771827] |
ChEMBL | Inhibition of wild type HIV1 protease expressed in Escherichia coli using Arg-Glu (EDANS)-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-Lys(DABCYL)-Arg as substrate preincubated for 20 to 30 mins followed by substrate addition and measured for 10 mins by FRET assay | B | 8.82 | pIC50 | 1.52 | nM | IC50 | Eur J Med Chem (2021) 220: 113498-113498 [PMID:33933756] |
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] | ||||||||
ChEMBL | Inhibition of human MDR1-dependent accumulation of calcein-AM expressed in MDCK2 cells | B | 4 | pIC50 | >100000 | nM | IC50 | Antimicrob Agents Chemother (2007) 51: 3498-3504 [PMID:17664327] |
ChEMBL | Inhibition of P-gp in human 12D7-MDR cells using NBD-Aba as substrate after 30 mins by flow cytometric analysis | B | 4.22 | pIC50 | 60000 | nM | IC50 | J Med Chem (2020) 63: 2131-2138 [PMID:31505928] |
ChEMBL | Inhibition of P-gp in human 12D7-MDR cells using calcein-AM as substrate after 30 mins by flow cytometric analysis | B | 4.48 | pIC50 | 33200 | nM | IC50 | J Med Chem (2020) 63: 2131-2138 [PMID:31505928] |
ChEMBL | Inhibition of P-gp in human CMEC/D3 cells using NBD-Aba as substrate after 30 mins by flow cytometric analysis | B | 4.81 | pIC50 | 15400 | nM | IC50 | J Med Chem (2020) 63: 2131-2138 [PMID:31505928] |
ChEMBL | Inhibition of P-gp in human CMEC/D3 cells using calcein-AM as substrate after 30 mins by flow cytometric analysis | B | 5.18 | pIC50 | 6600 | nM | IC50 | J Med Chem (2020) 63: 2131-2138 [PMID:31505928] |
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
ChEMBL | DNDI: Malaria in Vitro, 72 hour | F | 4.33 | pIC50 | 46930 | nM | IC50 | Antiprotozoal Activity Profiling of Approved Drugs: A Starting Point toward Drug Repositioning |
ChEMBL | Antimicrobial activity against chloroquine-resistant Plasmodium falciparum Dd2 after 48 hrs | F | 4.15 | pEC50 | 70000 | nM | EC50 | Antimicrob Agents Chemother (2010) 54: 1334-1337 [PMID:20028821] |
Protease in Human immunodeficiency virus 1 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366517] [UniProtKB: Q9YQ12] | ||||||||
ChEMBL | Binding affinity to HIV1 protease | B | 10.8 | pKd | 0.02 | nM | Kd | J Med Chem (2016) 59: 4171-4188 [PMID:26356253] |
ChEMBL | Inhibition of wild type HIV1 protease by competitive binding | B | 7.66 | pKi | 22 | nM | Ki | J Med Chem (2008) 51: 6599-6603 [PMID:18808097] |
ChEMBL | Inhibition of wild type HIV1 protease by uncompetitive binding | B | 7.74 | pKi | 18 | nM | Ki | J Med Chem (2008) 51: 6599-6603 [PMID:18808097] |
ChEMBL | Inhibition of wild type HIV1 protease by enzyme inhibition | B | 8.05 | pKi | 9 | nM | Ki | J Med Chem (2008) 51: 6599-6603 [PMID:18808097] |
ChEMBL | Inhibition of HIV1 protease expressed in Escherichia coli by fluorometric assay | B | 8.96 | pKi | 1.1 | nM | Ki | J Med Chem (2010) 53: 607-615 [PMID:19961222] |
ChEMBL | Inhibition of HIV1 recombinant protease using Lys-Ala-Arg-Val-Nle-Nph-Glu-Ala-Nle-NH2 as substrate by spectrophotometric analysis | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (2012) 55: 5784-5796 [PMID:22621689] |
ChEMBL | Inhibition of wild type HIV1 protease | B | 9.47 | pKi | 0.34 | nM | Ki | J Med Chem (2007) 50: 4509-4515 [PMID:17696515] |
ChEMBL | Binding affinity to HIV1 protease I50V mutant | B | 9.48 | pKi | 0.33 | nM | Ki | J Med Chem (2016) 59: 2849-2878 [PMID:26509831] |
ChEMBL | Inhibition of HIV1 NL4-3 protease I50V/A71V mutant expressed in Escherichia coli TAP-106 cells using EDANS/DABCYL-labelled 10-amino acid containing protease cleavage site as substrate preincubated for 1 hr followed by substrate addition and measured for 60 mins by FRET assay | B | 10.12 | pKi | 0.07 | nM | Ki | J Med Chem (2020) 63: 8296-8313 [PMID:32672965] |
ChEMBL | Inhibition of HIV1 NL4-3 protease I50V/A71V mutant expressed in Escherichia coli TAP-106 cells using EDANS/DABCYL-labelled 10-amino acid containing natural MA/CA cleavage site as substrate preincubated for 1 hr followed by substrate addition and measured for 60 mins by FRET assay | B | 10.12 | pKi | 0.07 | nM | Ki | J Med Chem (2019) 62: 8062-8079 [PMID:31386368] |
ChEMBL | Binding affinity to HIV1 protease D30N mutant | B | 10.39 | pKi | 0.04 | nM | Ki | J Med Chem (2016) 59: 2849-2878 [PMID:26509831] |
ChEMBL | Binding affinity to HIV1 protease N88D mutant | B | 10.39 | pKi | 0.04 | nM | Ki | J Med Chem (2016) 59: 2849-2878 [PMID:26509831] |
ChEMBL | Binding affinity to HIV1 protease A71V mutant | B | 10.6 | pKi | 0.03 | nM | Ki | J Med Chem (2016) 59: 2849-2878 [PMID:26509831] |
ChEMBL | Inhibition of HIV1 NL4-3 protease I84V mutant expressed in Escherichia coli TAP-106 cells using EDANS/DABCYL-labelled 10-amino acid containing natural MA/CA cleavage site as substrate preincubated for 1 hr followed by substrate addition and measured for 60 mins by FRET assay | B | 10.6 | pKi | 0.03 | nM | Ki | J Med Chem (2019) 62: 8062-8079 [PMID:31386368] |
ChEMBL | Binding affinity to HIV1 protease G73S mutant | B | 10.6 | pKi | 0.03 | nM | Ki | J Med Chem (2016) 59: 2849-2878 [PMID:26509831] |
ChEMBL | Inhibition of HIV1 NL4-3 protease I84V mutant expressed in Escherichia coli TAP-106 cells using EDANS/DABCYL-labelled 10-amino acid containing protease cleavage site as substrate preincubated for 1 hr followed by substrate addition and measured for 60 mins by FRET assay | B | 10.6 | pKi | 0.03 | nM | Ki | J Med Chem (2020) 63: 8296-8313 [PMID:32672965] |
ChEMBL | Binding affinity to HIV1 protease I84V mutant | B | 10.6 | pKi | 0.03 | nM | Ki | J Med Chem (2016) 59: 2849-2878 [PMID:26509831] |
ChEMBL | Binding affinity to HIV1 protease L90M mutant | B | 10.6 | pKi | 0.03 | nM | Ki | J Med Chem (2016) 59: 2849-2878 [PMID:26509831] |
ChEMBL | Inhibition of wild type HIV-1 NL4-3 protease expressed in Escherichia coli Rosetta (DE3)pLysS using Ac-Thr-Ile-Nle-Nle-Gln-Arg-NH2 as substrate by fluorescence assay | B | 10.8 | pKi | 0.02 | nM | Ki | J Med Chem (2018) 61: 4561-4577 [PMID:29763303] |
ChEMBL | Inhibition of HIV1 wild type NL4-3 protease expressed in Escherichia coli Rosetta (DE3) pLysS using Abz-Thr-Ile-Nle-Phe-(pNO2)-Gln-Arg-NH2 as substrate preincubated for 5 to 10 mins followed by substrate addition measured after 1 hr by fluorescence assay | B | 10.8 | pKi | 0.02 | nM | Ki | J Med Chem (2018) 61: 9722-9737 [PMID:30354121] |
ChEMBL | Inhibition of HIV1 protease | B | 10.8 | pKi | 0.02 | nM | Ki | Bioorg Med Chem (2007) 15: 7576-7580 [PMID:17900913] |
ChEMBL | Inhibition of HIV1 protease using Ac-Thr-Ile-Nle-Nle-Gln-Arg-NH2 substrate by continuous fluorometric assay | B | 10.8 | pKi | 0.02 | nM | Ki | Bioorg Med Chem Lett (2019) 29: 2565-2570 [PMID:31416666] |
ChEMBL | Inhibition of HIV-1 protease | B | 10.8 | pKi | 0.02 | nM | Ki | J Med Chem (2020) 63: 4867-4879 [PMID:32348139] |
ChEMBL | Inhibition of HIV1 protease | B | 10.8 | pKi | 0.02 | nM | Ki | J Med Chem (2009) 52: 7689-7705 [PMID:19746963] |
ChEMBL | Inhibition of HIV1 protease | B | 10.8 | pKi | 0.02 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 1241-1246 [PMID:20034787] |
ChEMBL | Inhibition of HIV1 protease | B | 10.8 | pKi | 0.02 | nM | Ki | J Med Chem (2012) 55: 3387-3397 [PMID:22401672] |
ChEMBL | Inhibition of HIV1 protease | B | 10.8 | pKi | 0.02 | nM | Ki | J Med Chem (2008) 51: 6021-6033 [PMID:18783203] |
ChEMBL | Inhibition of HIV1 protease | B | 10.8 | pKi | 0.02 | nM | Ki | J Med Chem (2012) 55: 5784-5796 [PMID:22621689] |
ChEMBL | Inhibition of HIV1 protease | B | 10.8 | pKi | 0.02 | nM | Ki | J Med Chem (2015) 58: 6994-7006 [PMID:26306007] |
ChEMBL | Inhibition of HIV-1 protease by fluorometric assay | B | 10.8 | pKi | 0.02 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 4903-4909 [PMID:26096678] |
ChEMBL | Inhibition of HIV1 protease dimerization in MT2 cells | B | 10.8 | pKi | 0.02 | nM | Ki | J Biol Chem (2007) 282: 28709-28720 [PMID:17635930] |
ChEMBL | Inhibition of HIV1 protease | B | 10.85 | pKi | 0.01 | nM | Ki | J Med Chem (2009) 52: 2163-2176 [PMID:19323561] |
ChEMBL | Inhibition of HIV1 protease using RE(Edans)SGIFLETSK(Dabcyl)R as substrate by fluorescence method | B | 11 | pKi | 0.01 | nM | Ki | J Med Chem (2019) 62: 9375-9414 [PMID:31050421] |
ChEMBL | Inhibition of wild type HIV1 protease expressed in Escherichia coli using Arg-Glu (EDANS)-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-Lys(DABCYL)-Arg as substrate preincubated for 20 to 30 mins followed by substrate addition and measured for 10 mins by FRET assay | B | 8.4 | pIC50 | 4.01 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 1541-1545 [PMID:31014912] |
ChEMBL | Inhibition of Human immunodeficiency virus 1 3B protease | B | 8.42 | pIC50 | 3.8 | nM | IC50 | ACS Med Chem Lett (2011) 2: 461-465 [PMID:24900331] |
ChEMBL | Inhibition of HIV1 protease expressed in Escherichia coli using Arg-Glu (EDANS)-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-Lys(DABCYL)-Arg as substrate preincubated for 20 to 30 mins followed by substrate addition and measured for 10 mins by FRET assay | B | 8.95 | pIC50 | 1.12 | nM | IC50 | Eur J Med Chem (2020) 185: 111866-111866 [PMID:31734023] |
ChEMBL | Inhibition of HIV1 protease expressed in Escherichia coli using Arg-Glu (EDANS)-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-Lys(DABCYL)-Arg as substrate preincubated for 20 to 30 mins followed by substrate addition and measured for 10 mins by FRET assay | B | 9.34 | pIC50 | 0.46 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 357-361 [PMID:30580917] |
ChEMBL | Inhibition of HIV1 protease expressed in Escherichia coli incubated for 20 to 30 mins at room temperature using (Arg-Glu(EDANS)-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-Lys(DABCYL)-Arg) substrate by FRET method | B | 10.21 | pIC50 | 0.06 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 1880-1883 [PMID:25838144] |
ChEMBL | Inhibition of HIV1 protease expressed in Escherichia coli using Arg-Glu (EDANS)-Ser-GlnAsn-Tyr-Pro-Ile-Val-Gln-Lys(DABCYL)-Arg as substrate preincubated for 20 to 30 mins followed by substrate addition measured for 10 mins by FRET method | B | 10.22 | pIC50 | 0.06 | nM | IC50 | Eur J Med Chem (2017) 137: 30-44 [PMID:28554091] |
ChEMBL | Inhibition of HIV1 protease expressed in Escherichia coli using Val-Ser-Gln-Asn-(beta-naphtyl)Ala-Pro-Ile-Val as substrate preincubated for 30 mins followed by substrate addition measured after 1 hr by mass spectrometric method | B | 10.89 | pIC50 | 0.01 | nM | IC50 | ACS Med Chem Lett (2017) 8: 1292-1297 [PMID:29259750] |
ChEMBL | Inhibition of DRV-resistant protease V32I/L33F/I54M/I84V mutant in HIV1 transfected in 293T cells after 48 hrs by lentiviral vector-based luciferase reporter gene assay | B | 6.95 | pEC50 | 112.08 | nM | EC50 | J Med Chem (2018) 61: 5138-5153 [PMID:29852069] |
ChEMBL | Inhibition of DRV-resistant protease V32I/L33F/I54M/V82I mutant in HIV1 transfected in 293T cells after 48 hrs by lentiviral vector-based luciferase reporter gene assay | B | 7.9 | pEC50 | 12.66 | nM | EC50 | J Med Chem (2018) 61: 5138-5153 [PMID:29852069] |
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 | pIC50 | 100000 | 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 | 4.4 | pIC50 | 39810.72 | 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 transfected with KCNQ1 / Kv1.7 / KvLQT1 and KCNE1/minK measured using IonWorks automated patch clamp platform | F | 4.3 | pIC50 | 50118.72 | 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] |
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]