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ChEMBL ligand: CHEMBL218490 (Dorzant, Dorzolamide, Dorzolamide, trans-(-)-, MK-507, Trusopt) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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AGAP002992-PA in Anopheles gambiae (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3399914] [UniProtKB: Q5TU56] | ||||||||
ChEMBL | Inhibition of Anopheles gambiae carbonic anhydrase pre-incubated for 15 mins by stopped-flow CO2 hydration assay | B | 6.56 | pKi | 275 | nM | Ki | Bioorg Med Chem (2015) 23: 2303-2309 [PMID:25882523] |
Alpha carbonic anhydrase in Stylophora pistillata (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075028] [UniProtKB: B5SU02] | ||||||||
ChEMBL | Inhibition of cloned Stylophora pistillata alpha-CA expressed in human HEK293 cells by stopped-flow CO2 assay | B | 7.74 | pKi | 18.1 | nM | Ki | Bioorg Med Chem (2009) 17: 5054-5058 [PMID:19520577] |
ChEMBL | Inhibition of Stylophora pistillata carbonic anhydrase by stopped-flow CO2 hydration assay | B | 7.74 | pKi | 18.1 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 710-714 [PMID:21208801] |
Androgen receptor/Androgen Receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275] | ||||||||
ChEMBL | Antagonist activity at recombinant human AR expressed in HEK293 cells assessed as inhibition of R1881-induced transcriptional activity measured after 24 hrs by dual luciferase reporter gene assay | B | 7.19 | pIC50 | 65 | nM | IC50 | J Med Chem (2020) 63: 12642-12665 [PMID:33095584] |
Androgen receptor/Androgen Receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207] | ||||||||
ChEMBL | Displacement of [3H]-MIB from wild-type rat AR LBD measured after 16 hrs by scintillation counting method | B | 7.96 | pKi | 11 | nM | Ki | J Med Chem (2020) 63: 12642-12665 [PMID:33095584] |
Astrosclerin-3 in Astrosclera willeyana (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1944499] [UniProtKB: A6YCJ1] | ||||||||
ChEMBL | Inhibition of GST-tagged astrosclera willeyana Astrosclerin-3 expressed in Escherichia coli after 15 mins preincubation by stopped flow CO2 hydration assay | B | 6.55 | pKi | 280 | nM | Ki | Bioorg Med Chem (2012) 20: 1403-1410 [PMID:22285172] |
Carbonate dehydratase in Sulfurihydrogenibium sp. (strain YO3AOP1) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3745586] [UniProtKB: B2V8E3] | ||||||||
ChEMBL | Inhibition of recombinant Sulfurihydrogenibium yellowstonense YO3AOP1 carbonic anhydrase by stopped flow CO2 hydrase assay | B | 8.1 | pKi | 8 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 401-405 [PMID:26691758] |
Carbonic anhydrase in Mycobacterium tuberculosis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6068] [UniProtKB: P9WPJ9] | ||||||||
ChEMBL | Inhibition of full length Mycobacterium tuberculosis H37Rv recombinant carbonic anhydrase 2 encoded by RV3588c by stopped flow CO2 hydration assay | B | 7 | pKi | 99 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 6649-6654 [PMID:19846301] |
Carbonic anhydrase in Methanosarcina thermophila (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3932] [UniProtKB: P40881] | ||||||||
ChEMBL | Inhibitory activity against alpha carbonic anhydrase (Co-Cam) from Methanosarcina thermophila | B | 5.77 | pKi | 1710 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 6001-6006 [PMID:15546717] |
ChEMBL | Inhibitory activity against alpha carbonic anhydrase (Zn-Cam) from Methanosarcina thermophila | B | 6.39 | pKi | 410 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 6001-6006 [PMID:15546717] |
Carbonic anhydrase in Stylophora pistillata (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1649055] [UniProtKB: C0IX24] | ||||||||
ChEMBL | Inhibition of Stylophora pistillata carbonic anhydrase 2 by stopped-flow CO2 hydration assay | B | 6.95 | pKi | 113 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 710-714 [PMID:21208801] |
Carbonic anhydrase in Methanobacterium thermoautotrophicum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3926] [UniProtKB: Q50565] | ||||||||
ChEMBL | Inhibitory activity against beta carbonic anhydrase (Cab) from Methanobacterium thermoautotrophicum | B | 4.51 | pKi | 30700 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 6001-6006 [PMID:15546717] |
Carbonic anhydrase in Candida albicans (strain SC5314 / ATCC MYA-2876) (Yeast) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5337] [UniProtKB: Q5AJ71] | ||||||||
ChEMBL | Inhibition of Candida albicans recombinant Nce103 by stopped-flow CO2 hydration assay | B | 6.05 | pKi | 887 | nM | Ki | Bioorg Med Chem (2009) 17: 4503-4509 [PMID:19450983] |
ChEMBL | Inhibition of Candida albicans CaNce103 preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method | B | 6.05 | pKi | 887 | nM | Ki | J Med Chem (2012) 55: 3513-3520 [PMID:22424239] |
Carbonic anhydrase in Candida glabrata CBS 138 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6185] [UniProtKB: Q6FTL6] | ||||||||
ChEMBL | Inhibition of recombinant full length Candida glabrata NCE103 expressed in Escherichia coli BL21 preincubated for 15 mins by stopped-flow CO2 hydrase assay | B | 5.18 | pKi | 6635 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 2647-2652 [PMID:23511020] |
Carbonic anhydrase in Saccharomyces cerevisiae S288c (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5931] [UniProtKB: P53615] | ||||||||
ChEMBL | Inhibition of Saccharomyces cerevisiae recombinant CA expressed in Escherichia coli by stopped-flow CO2 hydrase assay | B | 6.96 | pKi | 110 | nM | Ki | Bioorg Med Chem (2009) 17: 1158-1163 [PMID:19124253] |
Carbonic anhydrase 1 in Helicobacter pylori (strain ATCC 700392 / 26695) (Campylobacterpylori) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4211] [UniProtKB: O24855] | ||||||||
ChEMBL | Inhibition of Helicobacter pylori recombinant carbonic anhydrase by stopped-flow CO2 hydrase assay | B | 5.36 | pKi | 4360 | nM | Ki | J Med Chem (2006) 49: 2117-2126 [PMID:16539401] |
ChEMBL | Inhibition of Helicobacter pylori recombinant CA | B | 5.37 | pKi | 4310 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 2182-2188 [PMID:16459077] |
Carbonic anhydrase 15 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5973] [UniProtKB: Q99N23] | ||||||||
ChEMBL | Inhibition of mouse recombinant carbonic anhydrase 15 by stopped flow CO2 hydrase assay | B | 7.21 | pKi | 61 | nM | Ki | J Med Chem (2009) 52: 646-654 [PMID:19193158] |
Carbonic anhydrase 2 in Cryptococcus neoformans var. grubii (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1697676] [UniProtKB: Q3I4V7] | ||||||||
ChEMBL | Inhibition of Cryptococcus neoformans Can2 preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method | B | 5.08 | pKi | 8347 | nM | Ki | J Med Chem (2012) 55: 3513-3520 [PMID:22424239] |
Carbonic anhydrase, alpha family in Thiomicrospira crunogena (strain XCL-2) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3621035] [UniProtKB: Q31FD6] | ||||||||
ChEMBL | Inhibition of recombinant Thiomicrospira crunogena XCL-2 carbonic anhydrase by stopped flow CO2 hydrase assay | B | 8.15 | pKi | 7 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 401-405 [PMID:26691758] |
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 at 0.09 uM | B | 1.3 | pKi | 50000000 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 6001-6006 [PMID:15546717] |
ChEMBL | Inhibitory activity against human carbonic anhydrase I (hCAI) | B | 1.3 | pKi | 50000000 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 1149-1154 [PMID:15686931] |
GtoPdb | - | - | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 963-9 [PMID:15686894] |
ChEMBL | Inhibitory activity against human carbonic anhydrase I (hCA I) | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 2867-2873 [PMID:14611846] |
ChEMBL | Binding affinity against human carbonic anhydrase I (hCA I) | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1787-1791 [PMID:11425561] |
ChEMBL | Inhibition of cloned isozyme, human carbonic anhydrase I | B | 4.3 | pKi | >50000 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 575-582 [PMID:11229775] |
ChEMBL | Inhibition of human carbonic anhydrase I | B | 4.3 | pKi | >50000 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 225-229 [PMID:14684332] |
ChEMBL | Inhibition constant determined against human cloned carbonic anhydrase I | B | 4.3 | pKi | 50000 | nM | Ki | J Med Chem (2003) 46: 2187-2196 [PMID:12747790] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase I (CA1) | B | 4.3 | pKi | 50000 | nM | Ki | J Med Chem (2000) 43: 4542-4551 [PMID:11087579] |
ChEMBL | Inhibition of cloned human cytosolic isozyme Carbonic anhydrase I | B | 4.3 | pKi | 50000 | nM | Ki | J Med Chem (2004) 47: 1272-1279 [PMID:14971907] |
ChEMBL | Inhibitory activity against human cloned isoenzyme carbonic anhydrase I (hCA I), by esterase method. | B | 4.3 | pKi | >50000 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 837-840 [PMID:12617903] |
ChEMBL | Inhibitory activity against human cloned carbonic anhydrase isozyme I by esterase assay method. | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 1005-1009 [PMID:12643899] |
ChEMBL | Inhibitory activity against human carbonic anhydrase I | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 2351-2356 [PMID:15081039] |
ChEMBL | Inhibition of human cloned Carbonic anhydrase I | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 673-676 [PMID:10762051] |
ChEMBL | Inhibitory activity against human recombinant carbonic anhydrase I (CA1) | B | 4.3 | pKi | >50000 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 1551-1557 [PMID:12039560] |
ChEMBL | In vitro inhibitory activity against human carbonic anhydrase I (hCAI) | B | 4.3 | pKi | 50000 | nM | Ki | J Med Chem (2004) 47: 2796-2804 [PMID:15139757] |
ChEMBL | Inhibition of human carbonic anhydrase I (CAI) | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1117-1120 [PMID:10843231] |
ChEMBL | Inhibitory activity against human cloned carbonic anhydrase isozyme I (hCA I, cytosolic form). | B | 4.3 | pKi | 50000 | nM | Ki | J Med Chem (1999) 42: 2641-2650 [PMID:10411484] |
ChEMBL | Inhibitory activity against Human carbonic anhydrase I | B | 4.3 | pKi | >50000 | nM | Ki | J Med Chem (2002) 45: 1466-1476 [PMID:11906288] |
ChEMBL | Inhibitory activity against human recombinant carbonic anhydrase I (CA1) | B | 4.3 | pKi | 50000 | nM | Ki | J Med Chem (1999) 42: 3690-3700 [PMID:10479300] |
ChEMBL | Inhibitory activity against Carbonic anhydrase I | B | 4.3 | pKi | 50000 | nM | Ki | J Med Chem (2005) 48: 2121-2125 [PMID:15771455] |
ChEMBL | Inhibitory activity against human carbonic anhydrase I | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 3821-3827 [PMID:16039853] |
ChEMBL | Inhibitory activity against cytosolic human carbonic anhydrase I | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 579-584 [PMID:15664816] |
ChEMBL | Inhibitory potency against human cloned Carbonic anhydrase I expressed in Escherichia coli strain BL21 | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 367-372 [PMID:15603956] |
ChEMBL | Ki value against human carbonic anhydrase I | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 971-976 [PMID:15686895] |
ChEMBL | Ki value against human carbonic anhydrase I (hCA I) | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 963-969 [PMID:15686894] |
ChEMBL | Inhibitory activity against human carbonic anhydrase I expressed in Escherichia coli BL21 | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 5427-5433 [PMID:15454239] |
ChEMBL | Inhibitory activity against human Carbonic anhydrase I | B | 4.3 | pKi | 50000 | nM | Ki | J Med Chem (2004) 47: 5224-5229 [PMID:15456265] |
ChEMBL | Inhibitory constant against human Carbonic anhydrase I | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 3102-3108 [PMID:15905091] |
ChEMBL | Inhibitory activity against cloned human CA1 | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 437-442 [PMID:16290146] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 by stopped-flow CO2 hydrase assay | B | 4.3 | pKi | 50000 | nM | Ki | J Med Chem (2006) 49: 2117-2126 [PMID:16539401] |
ChEMBL | Inhibition of human recombinant CA1 | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 2182-2188 [PMID:16459077] |
ChEMBL | Inhibition of human cloned CA1 by stopped-flow CO2 hydration method | B | 4.3 | pKi | 50000 | nM | Ki | J Med Chem (2006) 49: 7024-7031 [PMID:17125255] |
ChEMBL | Inhibition of human recombinant cytosolic isozyme CA I by stopped-flow CO2 hydrase method | B | 4.3 | pKi | 50000 | nM | Ki | J Med Chem (2007) 50: 381-388 [PMID:17228881] |
ChEMBL | Inhibition of full length human cytosolic carbonic anhydrase 1 preincubated for 15 mins by stop flow CO2 hydrase assay | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 4184-4190 [PMID:27485387] |
ChEMBL | Inhibitory activity against human recombinant carbonic anhydrase I | B | 4.3 | pKi | 50000 | nM | Ki | J Med Chem (2000) 43: 4884-4892 [PMID:11123998] |
ChEMBL | Inhibition of human carbonic anhydrase-1 assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 secs by stopped-flow assay | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem (2017) 25: 3555-3561 [PMID:28511911] |
ChEMBL | Inhibition of recombinant human carbonic anhydrase 1 incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay | B | 4.3 | pKi | 50000 | nM | Ki | J Med Chem (2018) 61: 5380-5394 [PMID:29851481] |
ChEMBL | Inhibition of full length human CA 1 | B | 4.3 | pKi | 50000 | nM | Ki | Eur J Med Chem (2019) 168: 301-314 [PMID:30826507] |
ChEMBL | Inhibitory activity against human carbonic anhydrase I (hCA I) by using esterase assay method | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 3757-3762 [PMID:15203157] |
ChEMBL | Inhibition of human carbonic anhydrase 1 | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem (2007) 15: 4336-4350 [PMID:17475500] |
ChEMBL | Inhibition of human full length carbonic anhydrase 1 by stopped flow CO2 hydrase assay | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 2669-2674 [PMID:18359629] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydration method | B | 4.3 | pKi | 50000 | nM | Ki | J Med Chem (2009) 52: 2226-2232 [PMID:19317447] |
ChEMBL | Inhibition of human recombinant CA1 by stopped-flow CO2 hydrase assay | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem (2009) 17: 1158-1163 [PMID:19124253] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydrase assay | B | 4.3 | pKi | 50000 | nM | Ki | J Med Chem (2009) 52: 646-654 [PMID:19193158] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydration assay | B | 4.3 | pKi | 50000 | nM | Ki | J Med Chem (2009) 52: 3116-3120 [PMID:19338333] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 by stopped-flow CO2 hydrase method | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem (2009) 17: 4503-4509 [PMID:19450983] |
ChEMBL | Inhibition of human recombinant CA1 by stopped-flow CO2 assay | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem (2009) 17: 5054-5058 [PMID:19520577] |
ChEMBL | Inhibition of human full length cytosolic carbonic anhydrase 1 after 15 mins by stopped-flow CO2 hydration assay | B | 4.3 | pKi | 50000 | nM |