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Assay Detail

CHEMBL815970

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

Functional
Arbitary maximal response for cAMP elevation from baseline level was evaluated in Human U-937 cells
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type U-937
Confidence 1 — Organism
Curated By Expert

Target

U-937 (CHEMBL612794)
Type CELL-LINE
Organism Homo sapiens

Publication

7-Oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridines as novel inhibitors of human eosinophil phosphodiesterase.
Duplantier AJ, Andresen CJ, Cheng JB, Cohan VL, Decker C, DiCapua FM, Kraus KG, Johnson KL, Turner CR, UmLand JP, Watson JW, Wester RT, Williams AS, Williams JA.
J Med Chem (1998) 41 : 2268 -2277
PubMed 9632360 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 22 6.41 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL74597 1 9.00
CHEMBL308784 1 7.77
CHEMBL305806 1 7.44
CHEMBL310509 1 7.44
CHEMBL42126 PICLAMILAST 2.0 1 7.40
CHEMBL309803 1 7.39
CHEMBL307286 1 7.16
CHEMBL32442 CDP840 1 6.54
CHEMBL307678 1 6.48
CHEMBL75819 1 6.48
CHEMBL308180 1 6.30
CHEMBL75247 1 6.28
CHEMBL75722 1 6.11
CHEMBL73894 1 6.06
CHEMBL76066 1 6.01
CHEMBL63 ROLIPRAM 2.0 1 5.91
CHEMBL72688 1 5.49
CHEMBL511115 CILOMILAST 3.0 1 5.44
CHEMBL76065 1 5.28
CHEMBL74774 1 5.20
CHEMBL306335 1 4.96
CHEMBL307511 1 4.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL74597 EC50 = 1.0 nM 9.00
CHEMBL308784 EC50 = 17.0 nM 7.77
CHEMBL305806 EC50 = 36.0 nM 7.44
CHEMBL310509 EC50 = 36.0 nM 7.44
CHEMBL42126 PICLAMILAST EC50 = 40.0 nM 7.40
CHEMBL309803 EC50 = 41.0 nM 7.39
CHEMBL307286 EC50 = 70.0 nM 7.16
CHEMBL32442 CDP840 EC50 = 290.0 nM 6.54
CHEMBL307678 EC50 = 330.0 nM 6.48
CHEMBL75819 EC50 = 330.0 nM 6.48
CHEMBL308180 EC50 = 500.0 nM 6.30
CHEMBL75247 EC50 = 520.0 nM 6.28
CHEMBL75722 EC50 = 780.0 nM 6.11
CHEMBL73894 EC50 = 880.0 nM 6.06
CHEMBL76066 EC50 = 980.0 nM 6.01
CHEMBL63 ROLIPRAM EC50 = 1230.0 nM 5.91
CHEMBL72688 EC50 = 3210.0 nM 5.49
CHEMBL511115 CILOMILAST EC50 = 3630.0 nM 5.44
CHEMBL76065 EC50 = 5270.0 nM 5.28
CHEMBL74774 EC50 = 6250.0 nM 5.20
CHEMBL306335 EC50 = 11000.0 nM 4.96
CHEMBL307511 EC50 = 13000.0 nM 4.89