Reaction Details |
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Target | High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A |
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Ligand | BDBM50603811 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2245305 (CHEMBL5159515) |
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IC50 | 820±n/a nM |
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Citation | Song, Z; Huang, YY; Hou, KQ; Liu, L; Zhou, F; Huang, Y; Wan, G; Luo, HB; Xiong, XF Discovery and Structural Optimization of Toddacoumalone Derivatives as Novel PDE4 Inhibitors for the Topical Treatment of Psoriasis. J Med Chem65:4238-4254 (2022) [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 8A |
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Name: | High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A |
Synonyms: | High-affinity cAMP-specific and IBMX-insensitive 3 ,5 -cyclic phosphodiesterase 8A | PDE8A | PDE8A_HUMAN | Phosphodiesterase 8 | Phosphodiesterase 8 (PDE8) | Phosphodiesterase 8A (PDE8A) | Phosphodiesterase 8A (PDE8A1) | Phosphodiesterase 8A1 | Phosphodiesterase Type 8 (PDE8A) |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 93295.89 |
Organism: | Homo sapiens (Human) |
Description: | Recombinant catalytic domain (M1-E829) of human PDE8A. |
Residue: | 829 |
Sequence: | MGCAPSIHISERLVAEDAPSPAAPPLSSGGPRLPQGQKTAALPRTRGAGLLESELRDGSG
KKVAVADVQFGPMRFHQDQLQVLLVFTKEDNQCNGFCRACEKAGFKCTVTKEAQAVLACF
LDKHHDIIIIDHRNPRQLDAEALCRSIRSSKLSENTVIVGVVRRVDREELSVMPFISAGF
TRRYVENPNIMACYNELLQLEFGEVRSQLKLRACNSVFTALENSEDAIEITSEDRFIQYA
NPAFETTMGYQSGELIGKELGEVPINEKKADLLDTINSCIRIGKEWQGIYYAKKKNGDNI
QQNVKIIPVIGQGGKIRHYVSIIRVCNGNNKAEKISECVQSDTHTDNQTGKHKDRRKGSL
DVKAVASRATEVSSQRRHSSMARIHSMTIEAPITKVINIINAAQESSPMPVTEALDRVLE
ILRTTELYSPQFGAKDDDPHANDLVGGLMSDGLRRLSGNEYVLSTKNTQMVSSNIITPIS
LDDVPPRIARAMENEEYWDFDIFELEAATHNRPLIYLGLKMFARFGICEFLHCSESTLRS
WLQIIEANYHSSNPYHNSTHSADVLHATAYFLSKERIKETLDPIDEVAALIAATIHDVDH
PGRTNSFLCNAGSELAILYNDTAVLESHHAALAFQLTTGDDKCNIFKNMERNDYRTLRQG
IIDMVLATEMTKHFEHVNKFVNSINKPLATLEENGETDKNQEVINTMLRTPENRTLIKRM
LIKCADVSNPCRPLQYCIEWAARISEEYFSQTDEEKQQGLPVVMPVFDRNTCSIPKSQIS
FIDYFITDMFDAWDAFVDLPDLMQHLDNNFKYWKGLDEMKLRNLRPPPE
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BDBM50603811 |
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n/a |
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Name | BDBM50603811 |
Synonyms: | CHEMBL5171560 |
Type | Small organic molecule |
Emp. Form. | C21H28N2O3 |
Mol. Mass. | 356.4586 |
SMILES | [#6]-[#6]-n1c2nc(-[#6])ccc2c2-[#8][C@@]([#6])([#6]-[#6]-[#8])[#6]-[#6@@H](\[#6]=[#6](\[#6])-[#6])-c2c1=O |r| |
Structure |
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