Ki Summary

Reaction Details

Report a problem with these data

Target

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

Ligand

BDBM577145

Substrate/Competitor

n/a

Meas. Tech.

Scintillation Proximity Assay

IC50

2.99±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

BDBM577145

n/a

Name

BDBM577145

Synonyms:

4-(8-Cyclopropyl-9-oxo-6,7,8,9-tetrahydropyrido[2',3':4,5]pyrrolo[1,2-a]pyrazin-10-yl)-3-methylbenzonitrile | US11472805, Example 50

Type

Small organic molecule

Emp. Form.

C21H18N4O

Mol. Mass.

342.3938

SMILES

Cc1cc(ccc1-c1c2C(=O)N(CCn2c2cccnc12)C1CC1)C#N |(-3,.66,;-1.5,.98,;-1.02,2.44,;.5,2.81,;1.51,1.62,;1.04,.15,;-.47,-.17,;-.94,-1.63,;-.04,-2.88,;1.49,-3.04,;2.4,-1.79,;2.12,-4.45,;1.21,-5.69,;-.32,-5.53,;-.94,-4.12,;-2.41,-3.65,;-3.74,-4.42,;-5.08,-3.65,;-5.08,-2.11,;-3.74,-1.34,;-2.41,-2.11,;3.65,-4.61,;4.87,-5.55,;5.08,-4.02,;.98,4.28,;1.45,5.74,)|

Structure