Reaction Details |
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Target | Transient receptor potential cation channel subfamily M member 2 |
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Ligand | BDBM50505550 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1883243 (CHEMBL4384742) |
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IC50 | >30000±n/a nM |
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Citation | Pero, JE; Matthews, JM; Behm, DJ; Brnardic, EJ; Brooks, C; Budzik, BW; Costell, MH; Donatelli, CA; Eisennagel, SH; Erhard, K; Fischer, MC; Holt, DA; Jolivette, LJ; Li, H; Li, P; McAtee, JJ; McCleland, BW; Pendrak, I; Posobiec, LM; Rivera, KLK; Rivero, RA; Roethke, TJ; Sender, MR; Shu, A; Terrell, LR; Vaidya, K; Xu, X; Lawhorn, BG Design and Optimization of Sulfone Pyrrolidine Sulfonamide Antagonists of Transient Receptor Potential Vanilloid-4 with in Vivo Activity in a Pulmonary Edema Model. J Med Chem61:11209-11220 (2018) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Transient receptor potential cation channel subfamily M member 2 |
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Name: | Transient receptor potential cation channel subfamily M member 2 |
Synonyms: | EREG1 | Estrogen-responsive element-associated gene 1 protein | KNP3 | LTRPC2 | LTrpC-2 | Long transient receptor potential channel 2 | TRPC7 | TRPM2 | TRPM2_HUMAN | Transient receptor potential channel 7 |
Type: | PROTEIN |
Mol. Mass.: | 171218.39 |
Organism: | Homo sapiens (Human) |
Description: | ChEMBL_103516 |
Residue: | 1503 |
Sequence: | MEPSALRKAGSEQEEGFEGLPRRVTDLGMVSNLRRSNSSLFKSWRLQCPFGNNDKQESLS
SWIPENIKKKECVYFVESSKLSDAGKVVCQCGYTHEQHLEEATKPHTFQGTQWDPKKHVQ
EMPTDAFGDIVFTGLSQKVKKYVRVSQDTPSSVIYHLMTQHWGLDVPNLLISVTGGAKNF
NMKPRLKSIFRRGLVKVAQTTGAWIITGGSHTGVMKQVGEAVRDFSLSSSYKEGELITIG
VATWGTVHRREGLIHPTGSFPAEYILDEDGQGNLTCLDSNHSHFILVDDGTHGQYGVEIP
LRTRLEKFISEQTKERGGVAIKIPIVCVVLEGGPGTLHTIDNATTNGTPCVVVEGSGRVA
DVIAQVANLPVSDITISLIQQKLSVFFQEMFETFTESRIVEWTKKIQDIVRRRQLLTVFR
EGKDGQQDVDVAILQALLKASRSQDHFGHENWDHQLKLAVAWNRVDIARSEIFMDEWQWK
PSDLHPTMTAALISNKPEFVKLFLENGVQLKEFVTWDTLLYLYENLDPSCLFHSKLQKVL
VEDPERPACAPAAPRLQMHHVAQVLRELLGDFTQPLYPRPRHNDRLRLLLPVPHVKLNVQ
GVSLRSLYKRSSGHVTFTMDPIRDLLIWAIVQNRRELAGIIWAQSQDCIAAALACSKILK
ELSKEEEDTDSSEEMLALAEEYEHRAIGVFTECYRKDEERAQKLLTRVSEAWGKTTCLQL
ALEAKDMKFVSHGGIQAFLTKVWWGQLSVDNGLWRVTLCMLAFPLLLTGLISFREKRLQD
VGTPAARARAFFTAPVVVFHLNILSYFAFLCLFAYVLMVDFQPVPSWCECAIYLWLFSLV
CEEMRQLFYDPDECGLMKKAALYFSDFWNKLDVGAILLFVAGLTCRLIPATLYPGRVILS
LDFILFCLRLMHIFTISKTLGPKIIIVKRMMKDVFFFLFLLAVWVVSFGVAKQAILIHNE
RRVDWLFRGAVYHSYLTIFGQIPGYIDGVNFNPEHCSPNGTDPYKPKCPESDATQQRPAF
PEWLTVLLLCLYLLFTNILLLNLLIAMFNYTFQQVQEHTDQIWKFQRHDLIEEYHGRPAA
PPPFILLSHLQLFIKRVVLKTPAKRHKQLKNKLEKNEEAALLSWEIYLKENYLQNRQFQQ
KQRPEQKIEDISNKVDAMVDLLDLDPLKRSGSMEQRLASLEEQVAQTAQALHWIVRTLRA
SGFSSEADVPTLASQKAAEEPDAEPGGRKKTEEPGDSYHVNARHLLYPNCPVTRFPVPNE
KVPWETEFLIYDPPFYTAERKDAAAMDPMGDTLEPLSTIQYNVVDGLRDRRSFHGPYTVQ
AGLPLNPMGRTGLRGRGSLSCFGPNHTLYPMVTRWRRNEDGAICRKSIKKMLEVLVVKLP
LSEHWALPGGSREPGEMLPRKLKRILRQEHWPSFENLLKCGMEVYKGYMDDPRNTDNAWI
ETVAVSVHFQDQNDVELNRLNSNLHACDSGASIRWQVVDRRIPLYANHKTLLQKAAAEFG
AHY
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BDBM50505550 |
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n/a |
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Name | BDBM50505550 |
Synonyms: | CHEMBL4439190 | US11260049, Ex. 2 |
Type | Small organic molecule |
Emp. Form. | C18H16Cl2N2O6S2 |
Mol. Mass. | 491.365 |
SMILES | OC[C@]1(O)CN(C[C@@H]1S(=O)(=O)c1ccc(Cl)cc1)S(=O)(=O)c1ccc(cc1Cl)C#N |r| |
Structure |
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