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Assay Detail

CHEMBL768608

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

Binding
Inhibitory concentration against phosphodiesterase 4 (PDE4) in cytosol of human neutrophils
ChEMBL ↗
58
Total Activities
58
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

Novel selective PDE4 inhibitors. 3. In vivo antiinflammatory activity of a new series of N-substituted cis-tetra- and cis-hexahydrophthalazinones.
Van der Mey M, Boss H, Hatzelmann A, Van der Laan IJ, Sterk GJ, Timmerman H.
J Med Chem (2002) 45 : 2520 -2525
PubMed 12036360 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 58 7.88 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL315565 — — 1 9.40
CHEMBL82637 — — 1 9.30
CHEMBL81991 — — 1 9.30
CHEMBL314431 — — 1 9.20
CHEMBL82017 — — 1 9.20
CHEMBL315762 — — 1 9.20
CHEMBL85093 — — 1 9.10
CHEMBL314782 — — 1 9.10
CHEMBL84556 — — 1 9.00
CHEMBL315523 — — 1 8.90
CHEMBL86112 — — 1 8.90
CHEMBL315598 — — 1 8.90
CHEMBL82351 — — 1 8.60
CHEMBL85784 — — 1 8.60
CHEMBL86204 — — 1 8.50
CHEMBL85623 — — 1 8.40
CHEMBL84299 — — 1 8.20
CHEMBL441629 — — 1 8.10
CHEMBL420220 — — 1 8.10
CHEMBL81960 — — 1 8.10
CHEMBL84989 — — 1 8.00
CHEMBL313015 — — 1 8.00
CHEMBL85056 — — 1 8.00
CHEMBL84425 — — 1 8.00
CHEMBL87535 — — 1 7.90
CHEMBL312201 — — 1 7.90
CHEMBL314394 — — 1 7.90
CHEMBL83197 — — 1 7.90
CHEMBL84099 — — 1 7.80
CHEMBL83994 — — 1 7.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL315565 — IC50 = 0.3981 nM 9.40
CHEMBL82637 — IC50 = 0.5012 nM 9.30
CHEMBL81991 — IC50 = 0.5012 nM 9.30
CHEMBL314431 — IC50 = 0.631 nM 9.20
CHEMBL82017 — IC50 = 0.631 nM 9.20
CHEMBL315762 — IC50 = 0.631 nM 9.20
CHEMBL85093 — IC50 = 0.7943 nM 9.10
CHEMBL314782 — IC50 = 0.7943 nM 9.10
CHEMBL84556 — IC50 = 1.0 nM 9.00
CHEMBL315523 — IC50 = 1.259 nM 8.90
CHEMBL86112 — IC50 = 1.259 nM 8.90
CHEMBL315598 — IC50 = 1.259 nM 8.90
CHEMBL82351 — IC50 = 2.512 nM 8.60
CHEMBL85784 — IC50 = 2.512 nM 8.60
CHEMBL86204 — IC50 = 3.162 nM 8.50
CHEMBL85623 — IC50 = 3.981 nM 8.40
CHEMBL84299 — IC50 = 6.31 nM 8.20
CHEMBL441629 — IC50 = 7.943 nM 8.10
CHEMBL420220 — IC50 = 7.943 nM 8.10
CHEMBL81960 — IC50 = 7.943 nM 8.10
CHEMBL84989 — IC50 = 10.0 nM 8.00
CHEMBL313015 — IC50 = 10.0 nM 8.00
CHEMBL85056 — IC50 = 10.0 nM 8.00
CHEMBL84425 — IC50 = 10.0 nM 8.00
CHEMBL83197 — IC50 = 12.59 nM 7.90
CHEMBL312201 — IC50 = 12.59 nM 7.90
CHEMBL87535 — IC50 = 12.59 nM 7.90
CHEMBL314394 — IC50 = 12.59 nM 7.90
CHEMBL84099 — IC50 = 15.85 nM 7.80
CHEMBL83994 — IC50 = 15.85 nM 7.80
CHEMBL313272 — IC50 = 15.85 nM 7.80
CHEMBL419303 — IC50 = 19.95 nM 7.70
CHEMBL32442 CDP840 IC50 = 19.95 nM 7.70
CHEMBL314346 — IC50 = 25.12 nM 7.60
CHEMBL86267 — IC50 = 25.12 nM 7.60
CHEMBL85454 — IC50 = 25.12 nM 7.60
CHEMBL86239 — IC50 = 25.12 nM 7.60
CHEMBL83199 — IC50 = 25.12 nM 7.60
CHEMBL87577 — IC50 = 25.12 nM 7.60
CHEMBL86156 — IC50 = 25.12 nM 7.60
CHEMBL85941 — IC50 = 31.62 nM 7.50
CHEMBL313309 — IC50 = 31.62 nM 7.50
CHEMBL82263 — IC50 = 39.81 nM 7.40
CHEMBL82394 — IC50 = 39.81 nM 7.40
CHEMBL82695 — IC50 = 50.12 nM 7.30
CHEMBL430893 (-)-ROLIPRAM IC50 = 50.12 nM 7.30
CHEMBL316171 — IC50 = 63.1 nM 7.20
CHEMBL85940 — IC50 = 63.1 nM 7.20
CHEMBL85307 — IC50 = 79.43 nM 7.10
CHEMBL82393 — IC50 = 100.0 nM 7.00