dorzolamide [Ligand Id: 6810] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL218490 (Dorzant, Dorzolamide, Dorzolamide, trans-(-)-, MK-507, Trusopt)
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  • Alpha carbonic anhydrase in Stylophora pistillata [ChEMBL: CHEMBL1075028] [UniProtKB: B5SU02]
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  • Androgen receptor/Androgen Receptor in Human [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275]
  • Androgen receptor/Androgen Receptor in Rat [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
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  • Carbonate dehydratase in Sulfurihydrogenibium sp. (strain YO3AOP1) [ChEMBL: CHEMBL3745586] [UniProtKB: B2V8E3]
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  • Carbonic anhydrase in Mycobacterium tuberculosis [ChEMBL: CHEMBL6068] [UniProtKB: P9WPJ9]
  • Carbonic anhydrase in Methanosarcina thermophila [ChEMBL: CHEMBL3932] [UniProtKB: P40881]
  • Carbonic anhydrase in Stylophora pistillata [ChEMBL: CHEMBL1649055] [UniProtKB: C0IX24]
  • Carbonic anhydrase in Methanobacterium thermoautotrophicum [ChEMBL: CHEMBL3926] [UniProtKB: Q50565]
  • Carbonic anhydrase in Candida albicans (strain SC5314 / ATCC MYA-2876) (Yeast) [ChEMBL: CHEMBL5337] [UniProtKB: Q5AJ71]
  • Carbonic anhydrase in Candida glabrata CBS 138 [ChEMBL: CHEMBL6185] [UniProtKB: Q6FTL6]
  • Carbonic anhydrase in Saccharomyces cerevisiae S288c [ChEMBL: CHEMBL5931] [UniProtKB: P53615]
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  • Carbonic anhydrase 1 in Helicobacter pylori (strain ATCC 700392 / 26695) (Campylobacterpylori) [ChEMBL: CHEMBL4211] [UniProtKB: O24855]
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  • Carbonic anhydrase 2 in Cryptococcus neoformans var. grubii [ChEMBL: CHEMBL1697676] [UniProtKB: Q3I4V7]
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  • Carbonic anhydrase, alpha family in Thiomicrospira crunogena (strain XCL-2) [ChEMBL: CHEMBL3621035] [UniProtKB: Q31FD6]
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  • carbonic anhydrase 1/Carbonic anhydrase I in Human [ChEMBL: CHEMBL261] [GtoPdb: 2597] [UniProtKB: P00915]
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  • carbonic anhydrase 2/Carbonic anhydrase II in Human [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918]
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  • carbonic anhydrase 4/Carbonic anhydrase IV in Human [ChEMBL: CHEMBL3729] [GtoPdb: 2599] [UniProtKB: P22748]
  • Carbonic anhydrase IV in Bovine [ChEMBL: CHEMBL281] [UniProtKB: Q95323]
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  • carbonic anhydrase 9/Carbonic anhydrase IX in Human [ChEMBL: CHEMBL3594] [GtoPdb: 3055] [UniProtKB: Q16790]
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  • carbonic anhydrase 5A/Carbonic anhydrase VA in Human [ChEMBL: CHEMBL4789] [GtoPdb: 3093] [UniProtKB: P35218]
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  • carbonic anhydrase 7/Carbonic anhydrase VII in Human [ChEMBL: CHEMBL2326] [GtoPdb: 2749] [UniProtKB: P43166]
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  • carbonic anhydrase 12/Carbonic anhydrase XII in Human [ChEMBL: CHEMBL3242] [GtoPdb: 2747] [UniProtKB: O43570]
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  • carbonic anhydrase 13/Carbonic anhydrase XIII in Human [ChEMBL: CHEMBL3912] [GtoPdb: 2748] [UniProtKB: Q8N1Q1]
  • carbonic anhydrase 13/Carbonic anhydrase XIII in Mouse [ChEMBL: CHEMBL2186] [GtoPdb: 2748] [UniProtKB: Q9D6N1]
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  • carbonic anhydrase 14/Carbonic anhydrase XIV in Human [ChEMBL: CHEMBL3510] [GtoPdb: 2598] [UniProtKB: Q9ULX7]
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  • Delta carbonic anhydrase in Thalassiosira weissflogii [ChEMBL: CHEMBL3097982] [UniProtKB: Q5U9J1]
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  • PROBABLE TRANSMEMBRANE CARBONIC ANHYDRASE (CARBONATE DEHYDRATASE) (CARBONIC DEHYDRATASE) in Mycobacterium tuberculosis [ChEMBL: CHEMBL5767] [UniProtKB: P96878]
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  • Uncharacterized protein Rv1284/MT1322 in Mycobacterium tuberculosis [ChEMBL: CHEMBL5631] [UniProtKB: P9WPJ7]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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