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Target
Transient receptor potential cation channel subfamily M member 2
Ligand
BDBM50450500
Substrate
n/a
Meas. Tech.
ChEMBL_1742700 (CHEMBL4158450)
IC50
>10000±n/a nM
Citation
 Brnardic, EJ; Ye, G; Brooks, C; Donatelli, C; Barton, L; McAtee, J; Sanchez, RM; Shu, A; Erhard, K; Terrell, L; Graczyk-Millbrandt, G; He, Y; Costell, MH; Behm, DJ; Roethke, T; Stoy, P; Holt, DA; Lawhorn, BG Discovery of Pyrrolidine Sulfonamides as Selective and Orally Bioavailable Antagonists of Transient Receptor Potential Vanilloid-4 (TRPV4). J Med Chem 61:9738-9755 (2018) [PubMed]  Article 
Target
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:
MEPSALRKAGSEQEEGFEGLPRRVTDLGMVSNLRRSNSSLFKSWRLQCPFGNNDKQESLSSWIPENIKKKECVYFVESSKLSDAGKVVCQCGYTHEQHLEEATKPHTFQGTQWDPKKHVQEMPTDAFGDIVFTGLSQKVKKYVRVSQDTPSSVIYHLMTQHWGLDVPNLLISVTGGAKNFNMKPRLKSIFRRGLVKVAQTTGAWIITGGSHTGVMKQVGEAVRDFSLSSSYKEGELITIGVATWGTVHRREGLIHPTGSFPAEYILDEDGQGNLTCLDSNHSHFILVDDGTHGQYGVEIPLRTRLEKFISEQTKERGGVAIKIPIVCVVLEGGPGTLHTIDNATTNGTPCVVVEGSGRVADVIAQVANLPVSDITISLIQQKLSVFFQEMFETFTESRIVEWTKKIQDIVRRRQLLTVFREGKDGQQDVDVAILQALLKASRSQDHFGHENWDHQLKLAVAWNRVDIARSEIFMDEWQWKPSDLHPTMTAALISNKPEFVKLFLENGVQLKEFVTWDTLLYLYENLDPSCLFHSKLQKVLVEDPERPACAPAAPRLQMHHVAQVLRELLGDFTQPLYPRPRHNDRLRLLLPVPHVKLNVQGVSLRSLYKRSSGHVTFTMDPIRDLLIWAIVQNRRELAGIIWAQSQDCIAAALACSKILKELSKEEEDTDSSEEMLALAEEYEHRAIGVFTECYRKDEERAQKLLTRVSEAWGKTTCLQLALEAKDMKFVSHGGIQAFLTKVWWGQLSVDNGLWRVTLCMLAFPLLLTGLISFREKRLQDVGTPAARARAFFTAPVVVFHLNILSYFAFLCLFAYVLMVDFQPVPSWCECAIYLWLFSLVCEEMRQLFYDPDECGLMKKAALYFSDFWNKLDVGAILLFVAGLTCRLIPATLYPGRVILSLDFILFCLRLMHIFTISKTLGPKIIIVKRMMKDVFFFLFLLAVWVVSFGVAKQAILIHNERRVDWLFRGAVYHSYLTIFGQIPGYIDGVNFNPEHCSPNGTDPYKPKCPESDATQQRPAFPEWLTVLLLCLYLLFTNILLLNLLIAMFNYTFQQVQEHTDQIWKFQRHDLIEEYHGRPAAPPPFILLSHLQLFIKRVVLKTPAKRHKQLKNKLEKNEEAALLSWEIYLKENYLQNRQFQQKQRPEQKIEDISNKVDAMVDLLDLDPLKRSGSMEQRLASLEEQVAQTAQALHWIVRTLRASGFSSEADVPTLASQKAAEEPDAEPGGRKKTEEPGDSYHVNARHLLYPNCPVTRFPVPNEKVPWETEFLIYDPPFYTAERKDAAAMDPMGDTLEPLSTIQYNVVDGLRDRRSFHGPYTVQAGLPLNPMGRTGLRGRGSLSCFGPNHTLYPMVTRWRRNEDGAICRKSIKKMLEVLVVKLPLSEHWALPGGSREPGEMLPRKLKRILRQEHWPSFENLLKCGMEVYKGYMDDPRNTDNAWIETVAVSVHFQDQNDVELNRLNSNLHACDSGASIRWQVVDRRIPLYANHKTLLQKAAAEFGAHY
  
Inhibitor
Name:
BDBM50450500
Synonyms:
CHEMBL4164465
Type:
Small organic molecule
Emp. Form.:
C18H15Cl2FN2O5S
Mol. Mass.:
461.292
SMILES:
OC[C@]1(O)CN(C[C@@H]1Oc1ccc(C#N)c(F)c1)S(=O)(=O)c1ccc(Cl)cc1Cl |r|
Structure:
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