Ki Summary

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Target

Isoform 7 of cAMP-specific 3',5'-cyclic phosphodiesterase 4A (PDE4A8)

Ligand

BDBM399925

Substrate/Competitor

n/a

Meas. Tech.

cintillation Proximity Assay (SPA)

IC50

34.1±n/a nM

Citation

Chappie, TA; Patel, NC; Verhoest, PR; Helal, CJ; Sciabola, S; LaChapelle, EA; Wager, TT; Hayward, MM 6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-2-carboxamide compounds US Patent US10323042 Publication Date 6/18/2019

More Info.:

Get all data from this article, Assay Method

Isoform 7 of cAMP-specific 3',5'-cyclic phosphodiesterase 4A (PDE4A8)

Name:

Isoform 7 of cAMP-specific 3',5'-cyclic phosphodiesterase 4A (PDE4A8)

Synonyms:

Type:

Enzyme Catalytic Domain

Mol. Mass.:

91289.34

Organism:

Homo sapiens (Human)

Description:

P27815-7

Residue:

825

Sequence:

MRSGAAPRARPRPPALALPPTGPESLTHFPFSDEDTRRHPPGRSVSFEAENGPTPSPGRS
PLDSQASPGLVLHAGAATSQRRESFLYRSDSDYDMSPKTMSRNSSVTSEAHAEDLIVTPF
AQVLASLRSVRSNFSLLTNVPVPSNKRSPLGGPTPVCKATLSEETCQQLARETLEELDWC
LEQLETMQTYRSVSEMASHKFKRMLNRELTHLSEMSRSGNQVSEYISTTFLDKQNEVEIP
SPTMKEREKQQAPRPRPSQPPPPPVPHLQPMSQITGLKKLMHSNSLNNSNIPRFGVKTDQ
EELLAQELENLNKWGLNIFCVSDYAGGRSLTCIMYMIFQERDLLKKFRIPVDTMVTYMLT
LEDHYHADVAYHNSLHAADVLQSTHVLLATPALDAVFTDLEILAALFAAAIHDVDHPGVS
NQFLINTNSELALMYNDESVLENHHLAVGFKLLQEDNCDIFQNLSKRQRQSLRKMVIDMV
LATDMSKHMTLLADLKTMVETKKVTSSGVLLLDNYSDRIQVLRNMVHCADLSNPTKPLEL
YRQWTDRIMAEFFQQGDRERERGMEISPMCDKHTASVEKSQVGFIDYIVHPLWETWADLV
HPDAQEILDTLEDNRDWYYSAIRQSPSPPPEEESRGPGHPPLPDKFQFELTLEEEEEEEI
SMAQIPCTAQEALTAQGLSGVEEALDATIAWEASPAQESLEVMAQEASLEAELEAVYLTQ
QAQSTGSAPVAPDEFSSREEFVVAVSHSSPSALALQSPLLPAWRTLSVSEHAPGLPGLPS
TAAEVEAQREHQAAKRACSACAGTFGEDTSALPAPGGGGSGGDPT

BDBM399925

n/a

Name

BDBM399925

Synonyms:

3-(4-Cyano-5-fluoro-2-methylphenyl)-N-cyclopropyl-6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-2-carboxamide | US10323042, Example 5 | US10738063, Example 5

Type

Small organic molecule

Emp. Form.

C18H17FN4O2

Mol. Mass.

340.3516

SMILES

Cc1cc(C#N)c(F)cc1-c1c(nn2CCCOc12)C(=O)NC1CC1 |(-3.22,-18.2,;-1.72,-17.88,;-1.24,-16.42,;.28,-16.05,;.76,-14.58,;1.24,-13.12,;1.3,-17.24,;2.8,-16.92,;.82,-18.71,;-.68,-19.03,;-1.16,-20.49,;-.26,-21.74,;-1.16,-22.98,;-2.63,-22.51,;-3.96,-23.28,;-5.29,-22.51,;-5.29,-20.97,;-3.96,-20.2,;-2.63,-20.97,;1.28,-21.74,;2.05,-20.4,;2.05,-23.07,;3.59,-23.07,;4.93,-23.84,;4.93,-22.3,)|

Structure