Reaction Details |
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Target | cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A |
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Ligand | BDBM98990 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1437286 (CHEMBL3384789) |
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IC50 | 208±n/a nM |
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Citation | Rzasa, RM; Frohn, MJ; Andrews, KL; Chmait, S; Chen, N; Clarine, JG; Davis, C; Eastwood, HA; Horne, DB; Hu, E; Jones, AD; Kaller, MR; Kunz, RK; Miller, S; Monenschein, H; Nguyen, T; Pickrell, AJ; Porter, A; Reichelt, A; Zhao, X; Treanor, JJ; Allen, JR Synthesis and preliminary biological evaluation of potent and selective 2-(3-alkoxy-1-azetidinyl) quinolines as novel PDE10A inhibitors with improved solubility. Bioorg Med Chem22:6570-85 (2015) [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 |
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 |
Type: | Enzyme |
Mol. Mass.: | 124966.46 |
Organism: | Homo sapiens (Human) |
Description: | Q14432 |
Residue: | 1141 |
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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BDBM98990 |
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n/a |
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Name | BDBM98990 |
Synonyms: | US8497265, 446 |
Type | Small organic molecule |
Emp. Form. | C24H19N7O |
Mol. Mass. | 421.454 |
SMILES | Nc1ncc2cc(ccc2n1)-c1nccnc1OC1CN(C1)c1ccc2ccccc2n1 |
Structure |
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