Reaction Details |
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Target | High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B |
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Ligand | BDBM50390381 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_835072 (CHEMBL2073616) |
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IC50 | 43.9±n/a nM |
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Citation | DeNinno, MP; Wright, SW; Etienne, JB; Olson, TV; Rocke, BN; Corbett, JW; Kung, DW; DiRico, KJ; Andrews, KM; Millham, ML; Parker, JC; Esler, W; van Volkenburg, M; Boyer, DD; Houseknecht, KL; Doran, SD Discovery of triazolopyrimidine-based PDE8B inhibitors: exceptionally ligand-efficient and lipophilic ligand-efficient compounds for the treatment of diabetes. Bioorg Med Chem Lett22:5721-6 (2012) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B |
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Name: | High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B |
Synonyms: | PDE8B | PDE8B_HUMAN | Phosphodiesterase 8 | Phosphodiesterase 8B |
Type: | PROTEIN |
Mol. Mass.: | 98984.88 |
Organism: | Homo sapiens (Human) |
Description: | ChEMBL_876321 |
Residue: | 885 |
Sequence: | MGCAPSIHVSQSGVIYCRDSDESSSPRQTTSVSQGPAAPLPGLFVQTDAADAIPPSRASG
PPSVARVRRARTELGSGSSAGSAAPAATTSRGRRRHCCSSAEAETQTCYTSVKQVSSAEV
RIGPMRLTQDPIQVLLIFAKEDSQSDGFWWACDRAGYRCNIARTPESALECFLDKHHEII
VIDHRQTQNFDAEAVCRSIRATNPSEHTVILAVVSRVSDDHEEASVLPLLHAGFNRRFME
NSSIIACYNELIQIEHGEVRSQFKLRACNSVFTALDHCHEAIEITSDDHVIQYVNPAFER
MMGYHKGELLGKELADLPKSDKNRADLLDTINTCIKKGKEWQGVYYARRKSGDSIQQHVK
ITPVIGQGGKIRHFVSLKKLCCTTDNNKQIHKIHRDSGDNSQTEPHSFRYKNRRKESIDV
KSISSRGSDAPSLQNRRYPSMARIHSMTIEAPITKVINIINAAQENSPVTVAEALDRVLE
ILRTTELYSPQLGTKDEDPHTSDLVGGLMTDGLRRLSGNEYVFTKNVHQSHSHLAMPITI
NDVPPCISQLLDNEESWDFNIFELEAITHKRPLVYLGLKVFSRFGVCEFLNCSETTLRAW
FQVIEANYHSSNAYHNSTHAADVLHATAFFLGKERVKGSLDQLDEVAALIAATVHDVDHP
GRTNSFLCNAGSELAVLYNDTAVLESHHTALAFQLTVKDTKCNIFKNIDRNHYRTLRQAI
IDMVLATEMTKHFEHVNKFVNSINKPMAAEIEGSDCECNPAGKNFPENQILIKRMMIKCA
DVANPCRPLDLCIEWAGRISEEYFAQTDEEKRQGLPVVMPVFDRNTCSIPKSQISFIDYF
ITDMFDAWDAFAHLPALMQHLADNYKHWKTLDDLKCKSLRLPSDS
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BDBM50390381 |
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n/a |
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Name | BDBM50390381 |
Synonyms: | CHEMBL2070922 |
Type | Small organic molecule |
Emp. Form. | C16H14N8O |
Mol. Mass. | 334.3354 |
SMILES | Nc1nc(nc2n(Cc3nc4ccccc4c(=O)[nH]3)nnc12)C1CC1 |
Structure |
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