| Reaction Details |
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 | Report a problem with these data |
| Target | cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A |
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| Ligand | BDBM237920 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1612931 (CHEMBL3854731) |
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| IC50 | 14000±n/a nM |
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| Citation |  Cameron, KO; Kung, DW; Kalgutkar, AS; Kurumbail, RG; Miller, R; Salatto, CT; Ward, J; Withka, JM; Bhattacharya, SK; Boehm, M; Borzilleri, KA; Brown, JA; Calabrese, M; Caspers, NL; Cokorinos, E; Conn, EL; Dowling, MS; Edmonds, DJ; Eng, H; Fernando, DP; Frisbie, R; Hepworth, D; Landro, J; Mao, Y; Rajamohan, F; Reyes, AR; Rose, CR; Ryder, T; Shavnya, A; Smith, AC; Tu, M; Wolford, AC; Xiao, J Discovery and Preclinical Characterization of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy. J Med Chem59:8068-81 (2016) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A |
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| Name: | cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A |
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| Synonyms: | 3',5'-cyclic phosphodiesterase | CGI-PDE A | Cyclic GMP-inhibited phosphodiesterase A | PDE3A | PDE3A_HUMAN | Phosphodiesterase 3 | Phosphodiesterase 3 (PDE3) | Phosphodiesterase 3 and 5 (PDE3 and PDE5) | Phosphodiesterase 3A | Phosphodiesterase 3A (PDE3A) | Phosphodiesterase 3A (PDE3A1) | Phosphodiesterase Type 3 (PDE3A) | cGMP-inhibited 3',5'-cyclic phosphodiesterase A | cGMP-inhibited 3,5-cyclic phosphodiesterase A |
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| Type: | Enzyme |
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| Mol. Mass.: | 124966.46 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Q14432 |
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| Residue: | 1141 |
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| Sequence: | MAVPGDAARVRDKPVHSGVSQAPTAGRDCHHRADPASPRDSGCRGCWGDLVLQPLRSSRK
LSSALCAGSLSFLLALLVRLVRGEVGCDLEQCKEAAAAEEEEAAPGAEGGVFPGPRGGAP
GGGARLSPWLQPSALLFSLLCAFFWMGLYLLRAGVRLPLAVALLAACCGGEALVQIGLGV
GEDHLLSLPAAGVVLSCLAAATWLVLRLRLGVLMIALTSAVRTVSLISLERFKVAWRPYL
AYLAGVLGILLARYVEQILPQSAEAAPREHLGSQLIAGTKEDIPVFKRRRRSSSVVSAEM
SGCSSKSHRRTSLPCIPREQLMGHSEWDHKRGPRGSQSSGTSITVDIAVMGEAHGLITDL
LADPSLPPNVCTSLRAVSNLLSTQLTFQAIHKPRVNPVTSLSENYTCSDSEESSEKDKLA
IPKRLRRSLPPGLLRRVSSTWTTTTSATGLPTLEPAPVRRDRSTSIKLQEAPSSSPDSWN
NPVMMTLTKSRSFTSSYAISAANHVKAKKQSRPGALAKISPLSSPCSSPLQGTPASSLVS
KISAVQFPESADTTAKQSLGSHRALTYTQSAPDLSPQILTPPVICSSCGRPYSQGNPADE
PLERSGVATRTPSRTDDTAQVTSDYETNNNSDSSDIVQNEDETECLREPLRKASACSTYA
PETMMFLDKPILAPEPLVMDNLDSIMEQLNTWNFPIFDLVENIGRKCGRILSQVSYRLFE
DMGLFEAFKIPIREFMNYFHALEIGYRDIPYHNRIHATDVLHAVWYLTTQPIPGLSTVIN
DHGSTSDSDSDSGFTHGHMGYVFSKTYNVTDDKYGCLSGNIPALELMALYVAAAMHDYDH
PGRTNAFLVATSAPQAVLYNDRSVLENHHAAAAWNLFMSRPEYNFLINLDHVEFKHFRFL
VIEAILATDLKKHFDFVAKFNGKVNDDVGIDWTNENDRLLVCQMCIKLADINGPAKCKEL
HLQWTDGIVNEFYEQGDEEASLGLPISPFMDRSAPQLANLQESFISHIVGPLCNSYDSAG
LMPGKWVEDSDESGDTDDPEEEEEEAPAPNEEETCENNESPKKKTFKRRKIYCQITQHLL
QNHKMWKKVIEEEQRLAGIENQSLDQTPQSHSSEQIQAIKEEEEEKGKPRGEEIPTQKPD
Q
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| BDBM237920 |
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| n/a |
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| Name | BDBM237920 |
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| Synonyms: | US9394285, 1 |
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| Type | Small organic molecule |
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| Emp. Form. | C19H16ClNO3 |
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| Mol. Mass. | 341.788 |
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| SMILES | OC(=O)c1c[nH]c2cc(Cl)c(cc12)-c1ccc(cc1)C1(O)CCC1 |
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| Structure | 
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