Reaction Details |
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Target | cGMP-specific 3',5'-cyclic phosphodiesterase |
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Ligand | BDBM50525063 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1895394 (CHEMBL4397429) |
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IC50 | 5.3±n/a nM |
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Citation | Wang, Z; Jiang, X; Zhang, X; Tian, G; Yang, R; Wu, J; Zou, X; Liu, Z; Yang, X; Wu, C; Shi, J; Li, J; Suo, J; Wang, Y; Zhang, R; Xu, Z; Gong, X; He, Y; Zhu, W; Aisa, HA; Jiang, H; Xu, Y; Shen, J Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension. J Med Chem62:4979-4990 (2019) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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cGMP-specific 3',5'-cyclic phosphodiesterase |
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Name: | cGMP-specific 3',5'-cyclic phosphodiesterase |
Synonyms: | 3',5'-cyclic phosphodiesterase | CGB-PDE | PDE5 | PDE5A | PDE5A_HUMAN | Phosphodiesterase 2 and 5 (PDE2 and PDE5) | Phosphodiesterase 5 (PDE5) | Phosphodiesterase 5A | Phosphodiesterase 5A (PDE5A) | cGMP-binding cGMP-specific phosphodiesterase | cGMP-specific 3',5'-cyclic phosphodiesterase |
Type: | Protein |
Mol. Mass.: | 99975.83 |
Organism: | Homo sapiens (Human) |
Description: | O76074 |
Residue: | 875 |
Sequence: | MERAGPSFGQQRQQQQPQQQKQQQRDQDSVEAWLDDHWDFTFSYFVRKATREMVNAWFAE
RVHTIPVCKEGIRGHTESCSCPLQQSPRADNSAPGTPTRKISASEFDRPLRPIVVKDSEG
TVSFLSDSEKKEQMPLTPPRFDHDEGDQCSRLLELVKDISSHLDVTALCHKIFLHIHGLI
SADRYSLFLVCEDSSNDKFLISRLFDVAEGSTLEEVSNNCIRLEWNKGIVGHVAALGEPL
NIKDAYEDPRFNAEVDQITGYKTQSILCMPIKNHREEVVGVAQAINKKSGNGGTFTEKDE
KDFAAYLAFCGIVLHNAQLYETSLLENKRNQVLLDLASLIFEEQQSLEVILKKIAATIIS
FMQVQKCTIFIVDEDCSDSFSSVFHMECEELEKSSDTLTREHDANKINYMYAQYVKNTME
PLNIPDVSKDKRFPWTTENTGNVNQQCIRSLLCTPIKNGKKNKVIGVCQLVNKMEENTGK
VKPFNRNDEQFLEAFVIFCGLGIQNTQMYEAVERAMAKQMVTLEVLSYHASAAEEETREL
QSLAAAVVPSAQTLKITDFSFSDFELSDLETALCTIRMFTDLNLVQNFQMKHEVLCRWIL
SVKKNYRKNVAYHNWRHAFNTAQCMFAALKAGKIQNKLTDLEILALLIAALSHDLDHRGV
NNSYIQRSEHPLAQLYCHSIMEHHHFDQCLMILNSPGNQILSGLSIEEYKTTLKIIKQAI
LATDLALYIKRRGEFFELIRKNQFNLEDPHQKELFLAMLMTACDLSAITKPWPIQQRIAE
LVATEFFDQGDRERKELNIEPTDLMNREKKNKIPSMQVGFIDAICLQLYEALTHVSEDCF
PLLDGCRKNRQKWQALAEQQEKMLINGESGQAKRN
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BDBM50525063 |
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n/a |
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Name | BDBM50525063 |
Synonyms: | CHEMBL4522391 |
Type | Small organic molecule |
Emp. Form. | C17H23N3O2 |
Mol. Mass. | 301.3834 |
SMILES | CCCOc1ccc(N)cc1-c1nc(CC)c(CC)c(=O)[nH]1 |
Structure |
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