Reaction Details |
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Target | High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A |
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Ligand | BDBM50180268 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1583588 (CHEMBL3815675) |
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IC50 | >10000±n/a nM |
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Citation | Yoshikawa, M; Hitaka, T; Hasui, T; Fushimi, M; Kunitomo, J; Kokubo, H; Oki, H; Nakashima, K; Taniguchi, T Design and synthesis of potent and selective pyridazin-4(1H)-one-based PDE10A inhibitors interacting with Tyr683 in the PDE10A selectivity pocket. Bioorg Med Chem24:3447-55 (2016) [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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BDBM50180268 |
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n/a |
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Name | BDBM50180268 |
Synonyms: | CHEMBL3814662 |
Type | Small organic molecule |
Emp. Form. | C28H27N7O2 |
Mol. Mass. | 493.5597 |
SMILES | O=c1c(OCCN2CCn3c2nc2ccccc32)cn(CC2CC2)nc1-c1ccnn1-c1ccccc1 |
Structure |
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