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Cystic fibrosis transmembrane conductance regulator Inhibitors (IC50, Ki)

Structure
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Compound Name
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Standard Type
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Standard Values (in nM)
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12,14-Dimethyl-9-(5-methylfuran-2-yl)-17-phenyl-1,8,12,14-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-2,4,6,10,16-pentaene-13,15-dioneIC50250.0 [1]
CFTR(inh)-172IC50300.0 [1], 380.0 [2]
BPO-27 (racemate)IC508.0 [1], 40.0 [2]
9-(5-Bromofuran-2-yl)-12,14-dimethyl-17-phenyl-8-oxa-1,12,14-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-2,4,6,10,16-pentaene-13,15-dioneIC5090.0 [1], 200.0 [2]
9-(5-Bromofuran-2-yl)-12,14-dimethyl-4-nitro-17-phenyl-8-oxa-1,12,14-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-2(7),3,5,10,16-pentaene-13,15-dioneIC5025.0 [1], 120.0 [2]
12,14-Dimethyl-9-(5-methylfuran-2-yl)-4-nitro-17-phenyl-8-oxa-1,12,14-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-2(7),3,5,10,16-pentaene-13,15-dioneIC5025.0 [1], 100.0 [2]
Ethyl 9-(5-bromofuran-2-yl)-12,14-dimethyl-13,15-dioxo-17-phenyl-8-oxa-1,12,14-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-2(7),3,5,10,16-pentaene-4-carboxylateIC5025.0 [1], 50.0 [2]
9-(5-Bromofuran-2-yl)-12,14-dimethyl-17-phenyl-1,8,12,14-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-2,4,6,10,16-pentaene-13,15-dioneIC5050.0 [1], 90.0 [2]
9-(5-Iodofuran-2-yl)-12,14-dimethyl-17-phenyl-1,8,12,14-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-2,4,6,10,16-pentaene-13,15-dioneIC50100.0 [1], 170.0 [2]
GlyburideIC5015000.0 [1]
ApigeninKi81000.0 [1]
N-[(E)-(3,5-Dibromo-2,4-dihydroxyphenyl)methylideneamino]-2-(naphthalen-2-ylamino)acetamideIC505000.0 [1]
N-(2-(5-Chloro-2-methoxyphenylamino)-4'-methyl-4,5'-bithiazol-2'-yl)benzamideIC506000.0 [1]
2-(1-Hydroxypentyl)-6-methyl-3-(2-phenylethyl)-1H-Indole-5-carboxylic acidIC50160000.0 [1]
12,14-Dimethyl-9-(3-nitrophenyl)-17-phenyl-1,8,12,14-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-2,4,6,10,16-pentaene-13,15-dioneIC501200.0 [1]
4,5,12,14-Tetramethyl-9-(5-methylfuran-2-yl)-17-phenyl-1,8,12,14-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-2(7),3,5,10,16-pentaene-13,15-dioneIC50800.0 [1]
N-[12-(5-Chloro-2-methoxyanilino)-3,11-dithia-5,13-diazatricyclo[8.3.0.02,6]trideca-1(10),2(6),4,12-tetraen-4-yl]-2,2-dimethylpropanamideIC502300.0 [1]
2-((2-Carboxyethyl)carbamoyl)-6-methyl-3-phenethyl-1H-indole-5-carboxylic acidIC50490000.0 [1]
4-((4-Oxo-2-thioxo-3-(4-(trifluoromethyl)phenyl)thiazolidin-5-ylidene)methyl)benzoic acidIC5015000.0 [1]
3-(Hydroxymethyl)-5-methyl-2-pentyl-1-phenethyl-1H-indole-6-carboxylic acidIC50380000.0 [1]
N-[12-(5-Chloro-2-methoxyanilino)-3,11-dithia-5,13-diazatricyclo[8.3.0.02,6]trideca-1(10),2(6),4,12-tetraen-4-yl]cyclopropanecarboxamideIC508900.0 [1]
N-[12-(5-Chloro-2-methoxyanilino)-3,11-dithia-5,13-diazatricyclo[8.3.0.02,6]trideca-1(10),2(6),4,12-tetraen-4-yl]-2-methylpropanamideIC505800.0 [1]
N-[12-(5-Chloro-2-methoxyanilino)-3,11-dithia-5,13-diazatricyclo[8.3.0.02,6]trideca-1(10),2(6),4,12-tetraen-4-yl]-2-methylbutanamideIC506600.0 [1]
Methyl 4-[[12-(5-chloro-2-methoxyanilino)-3,11-dithia-5,13-diazatricyclo[8.3.0.02,6]trideca-1(10),2(6),4,12-tetraen-4-yl]amino]-4-oxobutanoateIC508800.0 [1]
N-[12-(5-Chloro-2-methoxyanilino)-3,11-dithia-5,13-diazatricyclo[8.3.0.02,6]trideca-1(10),2(6),4,12-tetraen-4-yl]-1,2-oxazole-5-carboxamideIC504800.0 [1]
N-[12-[5-Chloro-2-(dimethylamino)anilino]-3,11-dithia-5,13-diazatricyclo[8.3.0.02,6]trideca-1(10),2(6),4,12-tetraen-4-yl]-2,2-dimethylpropanamideIC506900.0 [1]
2,2-Dimethyl-N-[12-[(3-methylpyridin-2-yl)amino]-3,11-dithia-5,13-diazatricyclo[8.3.0.02,6]trideca-1(10),2(6),4,12-tetraen-4-yl]propanamideIC507200.0 [1]
N-[12-[3-(Dimethylamino)anilino]-3,11-dithia-5,13-diazatricyclo[8.3.0.02,6]trideca-1(10),2(6),4,12-tetraen-4-yl]-2,2-dimethylpropanamideIC502200.0 [1]
N-[12-(2-Methoxy-5-nitroanilino)-3,11-dithia-5,13-diazatricyclo[8.3.0.02,6]trideca-1(10),2(6),4,12-tetraen-4-yl]-2,2-dimethylpropanamideIC503600.0 [1]
2-(3-((4-Oxo-2-thioxo-3-(3-(trifluoromethyl)phenyl)thiazolidin-5-ylidene)methyl)phenoxy)acetic acidIC5030000.0 [1]
3-((4-Oxo-2-thioxo-3-(3-(trifluoromethyl)phenyl)thiazolidin-5-ylidene)methyl)benzoic acidIC501500.0 [1]
(Z)-5-(4-(1H-Tetrazol-5-yl)benzylidene)-2-thioxo-3-(3-(trifluoromethyl)phenyl)thiazolidin-4-oneIC50760.0 [1]
5-(4-(2H-Tetrazol-5-yl)benzylidene)-3-(3-(trifluoromethyl)phenyl)thiazolidine-2,4-dioneIC5017000.0 [1]
(2S,3S,4R)-3,4-Dihydroxy-2,4-dimethyl-3H-pyrimido[2,1-a]isoquinoline-2-carboxylic acidIC5015.0 [1]
(2R,4S,5R,6S)-2-Nonyl-6-phenyl-7-oxa-1-azabicyclo[3.2.1]octan-4-olIC5058620.0 [1]
(Z)-4-((3-(2,3-Dimethylphenyl)-4-oxo-2-thioxothiazolidin-5-ylidene)methyl)benzoic acidIC507000.0 [1]
5-(4-Pyridinylmethylene)-2-thioxo-3-[3-(trifluoromethyl)phenyl]-1,3-thiazolidin-4-oneIC5028000.0 [1]
4-[[4-Chloro-2,5-dioxo-1-[3-(trifluoromethyl)phenyl]pyrrol-3-yl]amino]benzoic acidIC5036000.0 [1]
2-(4-((4-Oxo-2-thioxo-3-(3-(trifluoromethyl)phenyl)thiazolidin-5-ylidene)methyl)phenoxy)acetic acidIC502600.0 [1]
(5Z)-5-(4-Hydroxybenzylidene)-2-thioxo-3-[3-(trifluoromethyl)phenyl]-1,3-thiazolidin-4-oneIC5024000.0 [1]
9-(3-Chlorophenyl)-17-(2-fluorophenyl)-12,14-dimethyl-1,8,12,14-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-2,4,6,10,16-pentaene-13,15-dioneIC502500.0 [1]
17-(2-Fluorophenyl)-4,5,12,14-tetramethyl-9-(5-methylfuran-2-yl)-1,8,12,14-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-2(7),3,5,10,16-pentaene-13,15-dioneIC501500.0 [1]
5-(3,5-Dibromo-4-hydroxybenzylidene)-2-thioxo-3-(3-(trifluoromethyl)phenyl)thiazolidin-4-oneIC507000.0 [1]
2-((4-Oxo-2-thioxo-3-(3-(trifluoromethyl)phenyl)thiazolidin-5-ylidene)methyl)benzoic acidIC5015000.0 [1]
9-(4-Hydroxyphenyl)-12,14-dimethyl-17-phenyl-1,8,12,14-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-2,4,6,10,16-pentaene-13,15-dioneIC504500.0 [1]
9-(2-Fluorophenyl)-12,14-dimethyl-17-phenyl-1,8,12,14-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-2,4,6,10,16-pentaene-13,15-dioneIC502000.0 [1]
9-(3-Methoxyphenyl)-12,14-dimethyl-17-(3-methylphenyl)-1,8,12,14-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-2,4,6,10,16-pentaene-13,15-dioneIC501700.0 [1]
9-(3-Fluorophenyl)-12,14-dimethyl-17-(3-methylphenyl)-1,8,12,14-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-2,4,6,10,16-pentaene-13,15-dioneIC508000.0 [1]
9-(2-Fluorophenyl)-12,14-dimethyl-17-(3-methylphenyl)-1,8,12,14-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-2,4,6,10,16-pentaene-13,15-dioneIC502500.0 [1]
12,14-Dimethyl-17-(2-methylphenyl)-9-phenyl-1,8,12,14-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-2,4,6,10,16-pentaene-13,15-dioneIC505000.0 [1]
12,14-Dimethyl-17-(2-methylphenyl)-9-(3-methylphenyl)-1,8,12,14-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-2,4,6,10,16-pentaene-13,15-dioneIC503000.0 [1]
9-(3-Methoxyphenyl)-12,14-dimethyl-17-(2-methylphenyl)-1,8,12,14-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-2,4,6,10,16-pentaene-13,15-dioneIC503000.0 [1]
9-(4-Hydroxyphenyl)-4,5,12,14-tetramethyl-17-phenyl-1,8,12,14-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-2(7),3,5,10,16-pentaene-13,15-dioneIC501500.0 [1]
4-((4-Oxo-2-thioxo-3-(2-(trifluoromethyl)phenyl)thiazolidin-5-ylidene)methyl)benzoic acidIC5012000.0 [1]
2-Hydroxy-5-((4-oxo-2-thioxo-3-(2-(trifluoromethyl)phenyl)thiazolidin-5-ylidene)methyl)benzoic acidIC5014000.0 [1]
2-(4-Carboxybutyl)-3-(hydroxymethyl)-5-methyl-1-(2-phenylethyl)indole-6-carboxylic acidIC50170000.0 [1]
12-N-(5-Chloro-2-methoxyphenyl)-3,11-dithia-5,13-diazatricyclo[8.3.0.02,6]trideca-1(10),2(6),4,12-tetraene-4,12-diamineIC5011000.0 [1]
N-[13-(5-Chloro-2-methoxyanilino)-3,12-dithia-5,14-diazatricyclo[9.3.0.02,6]tetradeca-1(11),2(6),4,13-tetraen-4-yl]-2,2-dimethylpropanamideIC504100.0 [1]
9-(3-Methoxyphenyl)-12,14-dimethyl-17-phenyl-1,8,12,14-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-2,4,6,10,16-pentaene-13,15-dioneIC501700.0 [1]
4-[2,5-Dioxo-1-[3-(trifluoromethyl)phenyl]pyrrolidin-3-yl]sulfanylbenzoic acidIC507000.0 [1]
2-Hydroxy-5-[(Z)-[4-oxo-2-sulfanylidene-3-[3-(trifluoromethyl)phenyl]-1,3-thiazolidin-5-ylidene]methyl]benzoic acidIC501400.0 [1]
(5Z)-2-Sulfanylidene-3-[3-(trifluoromethyl)phenyl]-5-[(3,4,5-trihydroxyphenyl)methylidene]-1,3-thiazolidin-4-oneIC5011000.0 [1]
4-((3-(4-Fluoro-3-(trifluoromethyl)phenyl)-4-oxo-2-thioxothiazolidin-5-ylidene)methyl)benzoic acidIC501500.0 [1]
4-((3-(4-Chloro-3-(trifluoromethyl)phenyl)-4-oxo-2-thioxothiazolidin-5-ylidene)methyl)benzoic acidIC5015000.0 [1]
4-((3-(3,5-Bis(trifluoromethyl)phenyl)-4-oxo-2-thioxothiazolidin-5-ylidene)methyl)benzoic acidIC5014000.0 [1]
3-((3-(4-Fluoro-3-(trifluoromethyl)phenyl)-4-oxo-2-thioxothiazolidin-5-ylidene)methyl)benzoic acidIC505000.0 [1]
4-[[4-Oxo-2-sulfanylidene-3-[3-(trifluoromethyl)phenyl]-1,3-thiazolidine-5-carbothioyl]amino]benzoic acidIC509000.0 [1]
5-(3,5-Dibromo-2,4-dihydroxybenzylidene)-2-thioxo-3-(3-(trifluoromethyl)phenyl)thiazolidin-4-oneIC508000.0 [1]
(5Z)-5-[(1-Oxidopyridin-1-ium-4-yl)methylidene]-2-sulfanylidene-3-[3-(trifluoromethyl)phenyl]-1,3-thiazolidin-4-oneIC508700.0 [1]
4-[[4-Oxo-2-thioxo-3-[2-methyl-3-(trifluoromethyl)phenyl]-5-thiazolidinylidene]methyl] benzoic acidIC508200.0 [1]
2-(4-Carboxy-1-hydroxybutyl)-6-methyl-3-(2-phenylethyl)-1H-indole-5-carboxylic acidIC50330000.0 [1]
2-Hydroxy-4-[[4-oxo-2-sulfanylidene-3-[3-(trifluoromethyl)phenyl]-1,3-thiazolidine-5-carbothioyl]amino]benzoic acidIC5025000.0 [1]
4-[[4-Oxo-2-sulfanylidene-3-[3-(trifluoromethyl)phenyl]-1,3-thiazolidin-5-yl]methyl]benzoic acidIC5027000.0 [1]
4-(4-(3-(Trifluoromethyl)phenyl)thiazol-2-ylamino)benzoic acidIC5028000.0 [1]
2-Hydroxy-5-(4-(3-(trifluoromethyl)phenyl)thiazol-2-ylamino)benzoic acidIC5032000.0 [1]
4-((4-Oxo-2-thioxo-3-m-tolylthiazolidin-5-ylidene)methyl)benzoic acidIC505000.0 [1]
3-((4-Oxo-2-thioxo-3-(4-(trifluoromethyl)phenyl)thiazolidin-5-ylidene)methyl)benzoic acidIC5013000.0 [1]
2-((4-Oxo-2-thioxo-3-(2-(trifluoromethyl)phenyl)thiazolidin-5-ylidene)methyl)benzoic acidIC5018000.0 [1]
3-((4-Oxo-2-thioxo-3-(2-(trifluoromethyl)phenyl)thiazolidin-5-ylidene)methyl)benzoic acidIC5019000.0 [1]
2-((4-Oxo-2-thioxo-3-(4-(trifluoromethyl)phenyl)thiazolidin-5-ylidene)methyl)benzoic acidIC5020000.0 [1]
4-[(Z)-[3-[2-Chloro-5-(trifluoromethyl)phenyl]-4-oxo-2-sulfanylidene-1,3-thiazolidin-5-ylidene]methyl]benzoic acidIC5020000.0 [1]
2-Hydroxy-5-((4-oxo-2-thioxo-3-(4-(trifluoromethyl)phenyl)thiazolidin-5-ylidene)methyl)benzoic acidIC5025000.0 [1]
(5Z)-2-Sulfanylidene-3-[3-(trifluoromethyl)phenyl]-5-[(2,3,4-trihydroxyphenyl)methylidene]-1,3-thiazolidin-4-oneIC5028000.0 [1]
12,14-Dimethyl-9-(5-methylfuran-2-yl)-17-(3-methylphenyl)-1,8,12,14-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-2,4,6,10,16-pentaene-13,15-dioneIC50700.0 [1]
12,14-Dimethyl-9,17-diphenyl-1,8,12,14-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-2,4,6,10,16-pentaene-13,15-dioneIC502500.0 [1]
9-(4-Hydroxy-2-methoxyphenyl)-12,14-dimethyl-17-phenyl-1,8,12,14-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-2,4,6,10,16-pentaene-13,15-dioneIC50100000.0 [1]
9-(2,3-Difluorophenyl)-12,14-dimethyl-17-phenyl-1,8,12,14-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-2,4,6,10,16-pentaene-13,15-dioneIC501200.0 [1]
9-(4-Hydroxyphenyl)-12,14-dimethyl-17-(3-methylphenyl)-1,8,12,14-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-2,4,6,10,16-pentaene-13,15-dioneIC501700.0 [1]
12,14-Dimethyl-17-(2-methylphenyl)-9-(3-nitrophenyl)-1,8,12,14-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-2,4,6,10,16-pentaene-13,15-dioneIC502000.0 [1]
12,14-Dimethyl-9-(5-methylfuran-2-yl)-17-(2-methylphenyl)-1,8,12,14-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-2,4,6,10,16-pentaene-13,15-dioneIC50800.0 [1]
17-(2-Fluorophenyl)-9-(3-methoxyphenyl)-12,14-dimethyl-1,8,12,14-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-2,4,6,10,16-pentaene-13,15-dioneIC502000.0 [1]
9-(2-Fluoro-3-nitrophenyl)-12,14-dimethyl-17-(3-methylphenyl)-1,8,12,14-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-2,4,6,10,16-pentaene-13,15-dioneIC502000.0 [1]
9-(5-Iodofuran-2-yl)-12,14-dimethyl-17-phenyl-8-oxa-1,12,14-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-2,4,6,10,16-pentaene-13,15-dioneIC50500.0 [1]
12,14-Dimethyl-9-(5-methylfuran-2-yl)-17-phenyl-8-oxa-1,12,14-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-2,4,6,10,16-pentaene-13,15-dioneIC50150.0 [1]
9-(5-Chlorofuran-2-yl)-12,14-dimethyl-17-(3-methylphenyl)-8-oxa-1,12,14-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-2,4,6,10,16-pentaene-13,15-dioneIC50370.0 [1]
12,14-Dimethyl-9-(5-methylfuran-2-yl)-17-(3-methylphenyl)-8-oxa-1,12,14-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-2,4,6,10,16-pentaene-13,15-dioneIC50600.0 [1]
9-(5-Bromofuran-2-yl)-12,14-dimethyl-4-nitro-17-phenyl-1,8,12,14-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-2(7),3,5,10,16-pentaene-13,15-dioneIC50170.0 [1]
4-Chloro-12,14-dimethyl-9-(5-methylfuran-2-yl)-5-nitro-17-phenyl-8-oxa-1,12,14-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-2,4,6,10,16-pentaene-13,15-dioneIC50170.0 [1]
Ethyl 12,14-dimethyl-9-(5-methylfuran-2-yl)-13,15-dioxo-17-phenyl-8-oxa-1,12,14-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-2(7),3,5,10,16-pentaene-4-carboxylateIC5080.0 [1]
12,14-Dimethyl-9-(5-methylfuran-2-yl)-8-nitroso-17-phenyl-1,8,12,14-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-2,4,6,10,16-pentaene-13,15-dioneIC502000.0 [1]
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References

This online tool may be cited as follows

MLA

"Quest Database™ Cystic fibrosis transmembrane conductance regulator Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 21 Feb. 2025, https://www.aatbio.com/data-sets/cystic-fibrosis-transmembrane-conductance-regulator-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2025, February 21). Quest Database™ Cystic fibrosis transmembrane conductance regulator Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/cystic-fibrosis-transmembrane-conductance-regulator-inhibitors-ic50-ki.
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