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Assay Detail

CHEMBL1048177

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

Binding
Inhibition of human recombinant PDE4B by scintillation proximity assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

3',5'-cyclic-AMP phosphodiesterase 4B (CHEMBL275)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Quinolines as a novel structural class of potent and selective PDE4 inhibitors. Optimisation for inhaled administration.
Woodrow MD, Ballantine SP, Barker MD, Clarke BJ, Dawson J, Dean TW, Delves CJ, Evans B, Gough SL, Guntrip SB, Holman S, Holmes DS, Kranz M, Lindvaal MK, Lucas FS, Neu M, Ranshaw LE, Solanke YE, Somers DO, Ward P, Wiseman JO.
Bioorg Med Chem Lett (2009) 19 : 5261 -5265
PubMed 19656678 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 8.52 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL569791 1 11.00
CHEMBL571381 1 10.70
CHEMBL584327 1 10.00
CHEMBL569556 1 9.90
CHEMBL193240 ROFLUMILAST 4.0 1 9.40
CHEMBL571171 1 9.20
CHEMBL576479 1 9.10
CHEMBL515240 1 8.80
CHEMBL570029 1 8.80
CHEMBL571593 1 8.70
CHEMBL585528 1 8.60
CHEMBL585937 1 8.50
CHEMBL571386 1 8.50
CHEMBL462150 1 8.40
CHEMBL569352 1 8.20
CHEMBL571594 1 8.00
CHEMBL569555 1 7.90
CHEMBL569790 1 7.60
CHEMBL570956 1 7.50
CHEMBL430893 (-)-ROLIPRAM 1 7.40
CHEMBL585537 1 7.40
CHEMBL571170 1 7.40
CHEMBL571383 1 6.80
CHEMBL576311 1 6.70
CHEMBL570015 GSK-256066 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL569791 IC50 = 0.01 nM 11.00
CHEMBL571381 IC50 = 0.01995 nM 10.70
CHEMBL584327 IC50 = 0.1 nM 10.00
CHEMBL569556 IC50 = 0.1259 nM 9.90
CHEMBL193240 ROFLUMILAST IC50 = 0.3981 nM 9.40
CHEMBL571171 IC50 = 0.631 nM 9.20
CHEMBL576479 IC50 = 0.7943 nM 9.10
CHEMBL515240 IC50 = 1.585 nM 8.80
CHEMBL570029 IC50 = 1.585 nM 8.80
CHEMBL571593 IC50 = 1.995 nM 8.70
CHEMBL585528 IC50 = 2.512 nM 8.60
CHEMBL585937 IC50 = 3.162 nM 8.50
CHEMBL571386 IC50 = 3.162 nM 8.50
CHEMBL462150 IC50 = 3.981 nM 8.40
CHEMBL569352 IC50 = 6.31 nM 8.20
CHEMBL571594 IC50 = 10.0 nM 8.00
CHEMBL569555 IC50 = 12.59 nM 7.90
CHEMBL569790 IC50 = 25.12 nM 7.60
CHEMBL570956 IC50 = 31.62 nM 7.50
CHEMBL430893 (-)-ROLIPRAM IC50 = 39.81 nM 7.40
CHEMBL585537 IC50 = 39.81 nM 7.40
CHEMBL571170 IC50 = 39.81 nM 7.40
CHEMBL571383 IC50 = 158.49 nM 6.80
CHEMBL576311 IC50 = 199.53 nM 6.70
CHEMBL570015 GSK-256066 IC50 = 0.007943 nM -