SC-560 [Ligand Id: 10240] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL26915 (SC-560) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| carbonic anhydrase 1/Carbonic anhydrase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL261] [GtoPdb: 2597] [UniProtKB: P00915] | ||||||||
| ChEMBL | Inhibitory activity against human carbonic anhydrase I was determined | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2004) 47: 550-557 [PMID:14736236] |
| carbonic anhydrase 2/Carbonic anhydrase II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918] | ||||||||
| ChEMBL | Inhibitory activity against human carbonic anhydrase II was determined | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2004) 47: 550-557 [PMID:14736236] |
| Carbonic anhydrase IV in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL281] [UniProtKB: Q95323] | ||||||||
| ChEMBL | Inhibitory activity against bovine carbonic anhydrase IV was determined | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2004) 47: 550-557 [PMID:14736236] |
| carbonic anhydrase 9/Carbonic anhydrase IX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3594] [GtoPdb: 3055] [UniProtKB: Q16790] | ||||||||
| ChEMBL | Inhibitory activity against human carbonic anhydrase IX was determined | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2004) 47: 550-557 [PMID:14736236] |
| COX-1 /Cyclooxygenase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219] | ||||||||
| ChEMBL | Inhibition of COX-1 in human OVCAR3 cells using [14C] arachidonic acid as substrate preincubated for 30 mins before substrate addition measured after 30 mins | B | 6.8 | pIC50 | 160 | nM | IC50 | J Med Chem (2012) 55: 2287-2300 [PMID:22263894] |
| ChEMBL | Inhibition of COX1 by microplate reader | B | 8 | pIC50 | 10 | nM | IC50 | J Nat Prod (2010) 73: 1234-1239 [PMID:20540535] |
| ChEMBL | Inhibition of COX1 | B | 8.05 | pIC50 | 9 | nM | IC50 | J Med Chem (2012) 55: 2287-2300 [PMID:22263894] |
| GtoPdb | - | - | 8.05 | pIC50 | 9 | nM | IC50 | Proc Natl Acad Sci USA (1998) 95: 13313-8 [PMID:9789085] |
| ChEMBL | Inhibition of COX1 in human blood assessed as PGE2 level incubated for 15 mins prior to LPS-challenge measured after 24 hrs by enzyme immunoassay | B | 8.05 | pIC50 | 8.9 | nM | IC50 | Bioorg Med Chem (2013) 21: 2355-2362 [PMID:23473947] |
| ChEMBL | Inhibition of COX1 in human OVCAR-3 cells assessed as reduction in PGE2 level incubated for 30 mins by ELISA | B | 8.1 | pIC50 | 8 | nM | IC50 | ACS Med Chem Lett (2021) 12: 798-804 [PMID:34055228] |
| ChEMBL | Inhibition of COX1 | B | 8.11 | pIC50 | 7.8 | nM | IC50 | Eur J Med Chem (2011) 46: 191-200 [PMID:21106277] |
| ChEMBL | In vitro inhibitory concentration required to block recombinant human prostaglandin G/H synthase 1 (COX-1) | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (1997) 40: 1347-1365 [PMID:9135032] |
| Cyclooxygenase-1 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2949] [UniProtKB: P05979] | ||||||||
| ChEMBL | Inhibition of ovine COX1 by peroxidase activity-based colorimetric assay | B | 7.11 | pIC50 | 77 | nM | IC50 | Eur J Med Chem (2014) 74: 606-618 [PMID:24531199] |
| ChEMBL | Inhibition of ovine recombinant COX1 assessed as decrease in formation of PGE2 using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition measured after 45 mins by LC-MS analysis | B | 7.41 | pIC50 | 39 | nM | IC50 | J Nat Prod (2019) 82: 3311-3320 [PMID:31774676] |
| ChEMBL | Inhibition of ovine COX1 using arachidonic acid as substrate pretreated for 5 mins followed by substrate addition and measured after 2 mins by fluorescence based enzyme immunoassay | B | 8 | pIC50 | 10 | nM | IC50 | Eur J Med Chem (2019) 180: 86-98 [PMID:31301566] |
| ChEMBL | Inhibition of recombinant ovine COX1 | B | 8 | pIC50 | 10 | nM | IC50 | ACS Med Chem Lett (2021) 12: 798-804 [PMID:34055228] |
| ChEMBL | Inhibition of ovine COX1 by fluorescence assay | B | 8.07 | pIC50 | 8.5 | nM | IC50 | Bioorg Med Chem (2012) 20: 2912-2922 [PMID:22475926] |
| ChEMBL | Inhibition of ovine COX-1 assessed as inhibition of PGH2 production using arachidonic acid as substrate by TMPD oxidation based colorimetric assay | B | 8.15 | pIC50 | 7 | nM | IC50 | Eur J Med Chem (2015) 94: 252-264 [PMID:25768707] |
| ChEMBL | Inhibition of ovine COX-1 assessed as reduction in PGE2 production using 10 uM arachidonic acid as substrate preincubated with enzyme for 5 mins followed by substrate addition and measured after 20 mins by ELISA | B | 8.22 | pIC50 | 6 | nM | IC50 | ACS Med Chem Lett (2021) 12: 610-616 [PMID:33854702] |
| COX-2 /Cyclooxygenase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354] | ||||||||
| ChEMBL | In vitro inhibitory concentration required to block human recombinant prostaglandin G/H synthase 2 (COX-2) | B | 4.13 | pIC50 | 74900 | nM | IC50 | J Med Chem (1997) 40: 1347-1365 [PMID:9135032] |
| ChEMBL | Inhibition of recombinant human COX2 | B | 4.25 | pIC50 | 55600 | nM | IC50 | ACS Med Chem Lett (2021) 12: 798-804 [PMID:34055228] |
| ChEMBL | Inhibition of recombinant human COX-2 preincubated for 15 mins followed by fluorometric substrate/heme addition for 15 mins subsequently incubated with arachidonic acid for 2 mins by fluorescence analysis | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2017) 60: 4135-4146 [PMID:28475316] |
| GtoPdb | - | - | 5.2 | pIC50 | 6300 | nM | IC50 | Proc Natl Acad Sci USA (1998) 95: 13313-8 [PMID:9789085] |
| ChEMBL | Inhibition of COX2 | B | 5.2 | pIC50 | 6300 | nM | IC50 | J Med Chem (2012) 55: 2287-2300 [PMID:22263894] |
| ChEMBL | Inhibition of recombinant human COX2 using arachidonic acid as substrate pretreated for 5 mins followed by substrate addition and measured after 2 mins by fluorescence based enzyme immunoassay | B | 5.48 | pIC50 | >3300 | nM | IC50 | Eur J Med Chem (2019) 180: 86-98 [PMID:31301566] |
| ChEMBL | Inhibition of human recombinant COX-2 assessed as reduction in PGE2 production using 10 uM arachidonic acid as substrate preincubated with enzyme for 5 mins followed by substrate addition and measured after 20 mins by ELISA | B | 5.99 | pIC50 | 1030 | nM | IC50 | ACS Med Chem Lett (2021) 12: 610-616 [PMID:33854702] |
| Cyclooxygenase-2 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4102] [UniProtKB: P79208] | ||||||||
| ChEMBL | Inhibition of ovine COX-2 assessed as inhibition of PGH2 production using arachidonic acid as substrate by TMPD oxidation based colorimetric assay | B | 4.13 | pIC50 | 74900 | nM | IC50 | Eur J Med Chem (2015) 94: 252-264 [PMID:25768707] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
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]
