Ki Summary

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Target

cAMP-specific 3',5'-cyclic phosphodiesterase 4A [2-825]

Ligand

BDBM577173

Substrate/Competitor

n/a

Meas. Tech.

Scintillation Proximity Assay

IC50

1.000±n/a nM

Citation

Chappie, TA; Patel, NC; Verhoest, PR; Helal, CJ; Sciabola, S; LaChapelle, EA; Wager, TT; Chandrasekaran, RY Tricyclic compounds and their use as phosphodiesterase inhibitors US Patent US11472805 Publication Date 10/18/2022

More Info.:

Get all data from this article, Assay Method

cAMP-specific 3',5'-cyclic phosphodiesterase 4A [2-825]

Name:

cAMP-specific 3',5'-cyclic phosphodiesterase 4A [2-825]

Synonyms:

DPDE2 | PDE4A | PDE4A_HUMAN | cAMP-specific 3',5'-cyclic phosphodiesterase (PDE4A3) (2-825)

Type:

Enzyme Catalytic Domain

Mol. Mass.:

92170.87

Organism:

Homo sapiens (Human)

Description:

aa 2-825

Residue:

824

Sequence:

EPPTVPSERSLSLSLPGPREGQATLKPPPQHLWRQPRTPIRIQQRGYSDSAERAERERQP
HRPIERADAMDTSDRPGLRTTRMSWPSSFHGTGTGSGGAGGGSSRRFEAENGPTPSPGRS
PLDSQASPGLVLHAGAATSQRRESFLYRSDSDYDMSPKTMSRNSSVTSEAHAEDLIVTPF
AQVLASLRSVRSNFSLLTNVPVPSNKRSPLGGPTPVCKATLSEETCQQLARETLEELDWC
LEQLETMQTYRSVSEMASHKFKRMLNRELTHLSEMSRSGNQVSEYISTTFLDKQNEVEIP
SPTMKEREKQQAPRPRPSQPPPPPVPHLQPMSQITGLKKLMHSNSLNNSNIPRFGVKTDQ
EELLAQELENLNKWGLNIFCVSDYAGGRSLTCIMYMIFQERDLLKKFRIPVDTMVTYMLT
LEDHYHADVAYHNSLHAADVLQSTHVLLATPALDAVFTDLEILAALFAAAIHDVDHPGVS
NQFLINTNSELALMYNDESVLENHHLAVGFKLLQEDNCDIFQNLSKRQRQSLRKMVIDMV
LATDMSKHMTLLADLKTMVETKKVTSSGVLLLDNYSDRIQVLRNMVHCADLSNPTKPLEL
YRQWTDRIMAEFFQQGDRERERGMEISPMCDKHTASVEKSQVGFIDYIVHPLWETWADLV
HPDAQEILDTLEDNRDWYYSAIRQSPSPPPEEESRGPGHPPLPDKFQFELTLEEEEEEEI
SMAQIPCTAQEALTAQGLSGVEEALDATIAWEASPAQESLEVMAQEASLEAELEAVYLTQ
QAQSTGSAPVAPDEFSSREEFVVAVSHSSPSALALQSPLLPAWR

BDBM577173

n/a

Name

BDBM577173

Synonyms:

10-(4-Chloro-2,5-difluorophenyl)-8-cyclopropyl-3,4,7,8-tetrahydro-2H-pyrano[2',3':4,5]pyrrolo[1,2-a]pyrazin-9(6H)-one | US11472805, Example 77

Type

Small organic molecule

Emp. Form.

C19H17ClF2N2O2

Mol. Mass.

378.8

SMILES

Fc1cc(-c2c3OCCCc3n3CCN(C4CC4)C(=O)c23)c(F)cc1Cl |(3.02,2.67,;1.51,2.35,;1.04,.89,;-.47,.57,;-.94,-.9,;-2.41,-1.38,;-3.74,-.61,;-5.08,-1.38,;-5.08,-2.92,;-3.74,-3.69,;-2.41,-2.92,;-.94,-3.39,;-.32,-4.8,;1.21,-4.96,;2.12,-3.71,;3.65,-3.87,;4.87,-4.82,;5.08,-3.29,;1.49,-2.31,;2.4,-1.06,;-.04,-2.15,;-1.5,1.71,;-3,1.39,;-1.02,3.17,;.48,3.49,;.96,4.96,)|

Structure