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Target
Transient receptor potential cation channel subfamily M member 2
Ligand
BDBM27497
Substrate
n/a
Meas. Tech.
ChEMBL_1719894 (CHEMBL4134894)
IC50
25±n/a nM
Citation
 Starkus, JG; Poerzgen, P; Layugan, K; Kawabata, KG; Goto, JI; Suzuki, S; Myers, G; Kelly, M; Penner, R; Fleig, A; Horgen, FD Scalaradial Is a Potent Inhibitor of Transient Receptor Potential Melastatin 2 (TRPM2) Ion Channels. J Nat Prod 80:2741-2750 (2017) [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:
BDBM27497
Synonyms:
2-(dimethylamino)-N-(6-oxo-5,6-dihydrophenanthridin-2-yl)acetamide | 2-Dimethylamino-N-(6-oxo-5,6-dihydro-phenanthridin-2-yl)-acetamide | CHEMBL372303 | N-(6-oxo-5,6-dihydro- phenanthridin-2-yl)-N,N-dimethylacetamide | N~2~,N~2~-DIMETHYL-N~1~-(6-OXO-5,6-DIHYDROPHENANTHRIDIN-2-YL)GLYCINAMIDE | PJ34
Type:
Small organic molecule
Emp. Form.:
C17H17N3O2
Mol. Mass.:
295.3358
SMILES:
CN(C)CC(=O)Nc1ccc2[nH]c(=O)c3ccccc3c2c1
Structure:
Search PDB for entries with ligand similarity: