Assay Detail

CHEMBL4339023

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Binding

Inhibition of PDE4 (unknown origin) by HTRF assay

ChEMBL ↗

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Target

Phosphodiesterase 4 (CHEMBL2093863) ↗

Open DB target context

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Phosphodiesterase 4 (CHEMBL2093863) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Phosphodiesterase 4

CHEMBL2093863

Anchored from Assay target.

Protein identity Phosphodiesterase 4

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Homo sapiens
Confidence	5 — Multiple protein complex / RNA
Curated By	Autocuration

Target

Phosphodiesterase 4 (CHEMBL2093863) ↗

Type	PROTEIN FAMILY
Organism	Homo sapiens

Publication

Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGFβR1 Inhibitor as an Immuno-oncology Agent.

Velaparthi U, Darne CP, Warrier J, Liu P, Rahaman H, Augustine-Rauch K, Parrish K, Yang Z, Swanson J, Brown J, Dhar G, Anandam A, Holenarsipur VK, Palanisamy K, Wautlet BS, Fereshteh MP, Lippy J, Tebben AJ, Sheriff S, Ruzanov M, Yan C, Gupta A, Gupta AK, Vetrichelvan M, Mathur A, Gelman M, Singh R, Kinsella T, Murtaza A, Fargnoli J, Vite G, Borzilleri RM.
ACS Med Chem Lett (2020) 11 : 172 -178
PubMed 32071685 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	4.96	4.96

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4514379	—	—	1	4.96

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4514379	—	IC50	=	11000.0	nM	4.96