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Assay Detail

CHEMBL846289

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

Binding
Affinity for rolipram binding site of phosphodiesterase type IV (PDE4)
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Phosphodiesterase 4 (CHEMBL2093863)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Orally active indole N-oxide PDE4 inhibitors.
Hulme C, Mathew R, Moriarty K, Miller B, Ramanjulu M, Cox P, Souness J, Page KM, Uhl J, Travis J, Labaudiniere R, Huang F, Djuric SW.
Bioorg Med Chem Lett (1998) 8 : 3053 -3058
PubMed 9873675 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 7.16 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42126 PICLAMILAST 2.0 1 9.40
CHEMBL63 ROLIPRAM 2.0 1 8.35
CHEMBL102635 1 7.92
CHEMBL102503 1 7.52
CHEMBL101479 1 7.52
CHEMBL102310 1 7.42
CHEMBL323069 1 7.29
CHEMBL102741 1 7.22
CHEMBL322837 1 7.19
CHEMBL414417 1 7.17
CHEMBL323132 1 7.17
CHEMBL103007 1 7.15
CHEMBL318586 1 7.07
CHEMBL102758 1 7.07
CHEMBL102876 1 6.94
CHEMBL299332 1 6.92
CHEMBL262269 1 6.87
CHEMBL301201 1 6.87
CHEMBL104780 1 6.65
CHEMBL321760 1 6.41
CHEMBL101368 1 5.95
CHEMBL102020 1 5.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42126 PICLAMILAST Ki = 0.4 nM 9.40
CHEMBL63 ROLIPRAM Ki = 4.5 nM 8.35
CHEMBL102635 Ki = 12.0 nM 7.92
CHEMBL102503 Ki = 30.0 nM 7.52
CHEMBL101479 Ki = 30.0 nM 7.52
CHEMBL102310 Ki = 38.0 nM 7.42
CHEMBL323069 Ki = 51.0 nM 7.29
CHEMBL102741 Ki = 60.0 nM 7.22
CHEMBL322837 Ki = 64.0 nM 7.19
CHEMBL414417 Ki = 67.0 nM 7.17
CHEMBL323132 Ki = 67.0 nM 7.17
CHEMBL103007 Ki = 71.0 nM 7.15
CHEMBL318586 Ki = 86.0 nM 7.07
CHEMBL102758 Ki = 86.0 nM 7.07
CHEMBL102876 Ki = 116.0 nM 6.94
CHEMBL299332 Ki = 120.0 nM 6.92
CHEMBL262269 Ki = 135.0 nM 6.87
CHEMBL301201 Ki = 135.0 nM 6.87
CHEMBL104780 Ki = 225.0 nM 6.65
CHEMBL321760 Ki = 393.0 nM 6.41
CHEMBL101368 Ki = 1124.0 nM 5.95
CHEMBL102020 Ki = 3184.0 nM 5.50