Reaction Details |
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Target | Cystic fibrosis transmembrane conductance regulator [1-507,509-1480] |
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Ligand | BDBM297408 |
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Substrate/Competitor | n/a |
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Meas. Tech. | Potentiator Assay |
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EC50 | 60.0±n/a nM |
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Citation | GRANT, SS; HEDERER, B; LANGENICKEL, T; ROWLANDS, DJ; STRIETER, RM; TIAN, X Pyridine and Pyrazine derivative for the Treatment of CF, COPD, and Bronchiectasis US Patent US20240058315 Publication Date 2/22/2024 |
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More Info.: | Get all data from this article, Assay Method |
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Cystic fibrosis transmembrane conductance regulator [1-507,509-1480] |
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Name: | Cystic fibrosis transmembrane conductance regulator [1-507,509-1480] |
Synonyms: | ABCC7 | CFTR | CFTR F508del | CFTR del508F | CFTR_HUMAN | Cystic fibrosis transmembrane conductance regulator (aa 1-507, aa 509-1480) |
Type: | Protein |
Mol. Mass.: | 168024.13 |
Organism: | Homo sapiens (Human) |
Description: | Human CTFR variant with F508 deletion. |
Residue: | 1479 |
Sequence: | MQRSPLEKASVVSKLFFSWTRPILRKGYRQRLELSDIYQIPSVDSADNLSEKLEREWDRE
LASKKNPKLINALRRCFFWRFMFYGIFLYLGEVTKAVQPLLLGRIIASYDPDNKEERSIA
IYLGIGLCLLFIVRTLLLHPAIFGLHHIGMQMRIAMFSLIYKKTLKLSSRVLDKISIGQL
VSLLSNNLNKFDEGLALAHFVWIAPLQVALLMGLIWELLQASAFCGLGFLIVLALFQAGL
GRMMMKYRDQRAGKISERLVITSEMIENIQSVKAYCWEEAMEKMIENLRQTELKLTRKAA
YVRYFNSSAFFFSGFFVVFLSVLPYALIKGIILRKIFTTISFCIVLRMAVTRQFPWAVQT
WYDSLGAINKIQDFLQKQEYKTLEYNLTTTEVVMENVTAFWEEGFGELFEKAKQNNNNRK
TSNGDDSLFFSNFSLLGTPVLKDINFKIERGQLLAVAGSTGAGKTSLLMVIMGELEPSEG
KIKHSGRISFCSQFSWIMPGTIKENIIGVSYDEYRYRSVIKACQLEEDISKFAEKDNIVL
GEGGITLSGGQRARISLARAVYKDADLYLLDSPFGYLDVLTEKEIFESCVCKLMANKTRI
LVTSKMEHLKKADKILILHEGSSYFYGTFSELQNLQPDFSSKLMGCDSFDQFSAERRNSI
LTETLHRFSLEGDAPVSWTETKKQSFKQTGEFGEKRKNSILNPINSIRKFSIVQKTPLQM
NGIEEDSDEPLERRLSLVPDSEQGEAILPRISVISTGPTLQARRRQSVLNLMTHSVNQGQ
NIHRKTTASTRKVSLAPQANLTELDIYSRRLSQETGLEISEEINEEDLKECFFDDMESIP
AVTTWNTYLRYITVHKSLIFVLIWCLVIFLAEVAASLVVLWLLGNTPLQDKGNSTHSRNN
SYAVIITSTSSYYVFYIYVGVADTLLAMGFFRGLPLVHTLITVSKILHHKMLHSVLQAPM
STLNTLKAGGILNRFSKDIAILDDLLPLTIFDFIQLLLIVIGAIAVVAVLQPYIFVATVP
VIVAFIMLRAYFLQTSQQLKQLESEGRSPIFTHLVTSLKGLWTLRAFGRQPYFETLFHKA
LNLHTANWFLYLSTLRWFQMRIEMIFVIFFIAVTFISILTTGEGEGRVGIILTLAMNIMS
TLQWAVNSSIDVDSLMRSVSRVFKFIDMPTEGKPTKSTKPYKNGQLSKVMIIENSHVKKD
DIWPSGGQMTVKDLTAKYTEGGNAILENISFSISPGQRVGLLGRTGSGKSTLLSAFLRLL
NTEGEIQIDGVSWDSITLQQWRKAFGVIPQKVFIFSGTFRKNLDPYEQWSDQEIWKVADE
VGLRSVIEQFPGKLDFVLVDGGCVLSHGHKQLMCLARSVLSKAKILLLDEPSAHLDPVTY
QIIRRTLKQAFADCTVILCEHRIEAMLECQQFLVIEENKVRQYDSIQKLLNERSLFRQAI
SPSDRVKLFPHRNSSKCKSKPQIAALKEETEEEVQDTRL
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BDBM297408 |
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n/a |
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Name | BDBM297408 |
Synonyms: | 3-Amino-6-(4-fluoro-phenyl)-5-trifluoromethyl-pyridine-2-carboxylic acid ((R)-3,3,3-trifluoro-2-hydroxy-2-methyl-propyl)-amide | US10117858, Example 8 | US20240058315, Example 8 |
Type | Small organic molecule |
Emp. Form. | C17H14F7N3O2 |
Mol. Mass. | 425.3008 |
SMILES | C[C@@](O)(CNC(=O)c1nc(-c2ccc(F)cc2)c(cc1N)C(F)(F)F)C(F)(F)F |r| |
Structure |
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