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Assay Detail

CHEMBL798530

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Binding affinity to rolipram binding site in isolated rat brain by rolipram binding assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Phosphodiesterase 4 (CHEMBL2094267)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Syntheses and evaluation of pyrido[2,3-dlpyrimidine-2,4-diones as PDE 4 inhibitors.
Nam G, Yoon CM, Kim E, Rhee CK, Kim JH, Shin JH, Kim SH.
Bioorg Med Chem Lett (2001) 11 : 611 -614
PubMed 11266153 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.36 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL63 ROLIPRAM 2.0 1 8.70
CHEMBL511115 CILOMILAST 3.0 1 6.75
CHEMBL347478 1 6.31
CHEMBL347429 1 6.12
CHEMBL157550 1 6.02
CHEMBL346928 1 6.00
CHEMBL157897 1 4.63
CHEMBL156054 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL63 ROLIPRAM IC50 = 2.0 nM 8.70
CHEMBL511115 CILOMILAST IC50 = 180.0 nM 6.75
CHEMBL347478 IC50 = 491.0 nM 6.31
CHEMBL347429 IC50 = 755.0 nM 6.12
CHEMBL157550 IC50 = 950.0 nM 6.02
CHEMBL346928 IC50 = 1010.0 nM 6.00
CHEMBL157897 IC50 = 23400.0 nM 4.63
CHEMBL156054 IC50 - nM -