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Assay Detail

CHEMBL989823

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

Binding
Inhibition of full length human PDE4D2 expressed in Escherichia coli BL21 by liquid scintillation counting
91
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

3',5'-cyclic-AMP phosphodiesterase 4D (CHEMBL288)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and structure-activity relationship, molecular modeling, and NMR studies of a series of phenyl alkyl ketones as highly potent and selective phosphodiesterase-4 inhibitors.
Zheng S, Kaur G, Wang H, Li M, Macnaughtan M, Yang X, Reid S, Prestegard J, Wang B, Ke H.
J Med Chem (2008) 51 : 7673 -7688
PubMed 19049349 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 91 5.68 7.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL458298 2 7.74
CHEMBL511686 2 7.66
CHEMBL45834 1 7.55
CHEMBL508134 2 7.21
CHEMBL47113 1 7.15
CHEMBL456591 2 6.75
CHEMBL457663 2 6.75
CHEMBL517124 1 6.70
CHEMBL456573 2 6.70
CHEMBL458297 2 6.46
CHEMBL457215 2 6.42
CHEMBL45055 1 6.40
CHEMBL456574 2 6.40
CHEMBL456590 2 6.39
CHEMBL456617 2 6.30
CHEMBL63 ROLIPRAM 2.0 2 6.26
CHEMBL458933 2 6.20
CHEMBL45854 1 6.19
CHEMBL458932 2 6.18
CHEMBL443679 2 6.14
CHEMBL457662 2 5.96
CHEMBL298000 1 5.80
CHEMBL456327 2 5.72
CHEMBL458931 2 5.66
CHEMBL516301 2 5.64
CHEMBL513099 2 5.59
CHEMBL460188 2 5.59
CHEMBL44109 1 5.51
CHEMBL456368 2 5.46
CHEMBL456618 2 5.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL458298 IC50 = 18.2 nM 7.74
CHEMBL511686 IC50 = 21.88 nM 7.66
CHEMBL458298 IC50 = 26.0 nM 7.58
CHEMBL45834 IC50 = 28.18 nM 7.55
CHEMBL511686 IC50 = 28.0 nM 7.55
CHEMBL508134 IC50 = 61.66 nM 7.21
CHEMBL508134 IC50 = 61.0 nM 7.21
CHEMBL47113 IC50 = 70.79 nM 7.15
CHEMBL457663 IC50 = 180.0 nM 6.75
CHEMBL456591 IC50 = 177.83 nM 6.75
CHEMBL457663 IC50 = 181.97 nM 6.74
CHEMBL456591 IC50 = 190.0 nM 6.72
CHEMBL517124 IC50 = 199.53 nM 6.70
CHEMBL456573 IC50 = 199.53 nM 6.70
CHEMBL456573 IC50 = 220.0 nM 6.66
CHEMBL458297 IC50 = 346.74 nM 6.46
CHEMBL458297 IC50 = 350.0 nM 6.46
CHEMBL457215 IC50 = 380.0 nM 6.42
CHEMBL457215 IC50 = 380.19 nM 6.42
CHEMBL45055 IC50 = 398.11 nM 6.40
CHEMBL456574 IC50 = 398.11 nM 6.40
CHEMBL456590 IC50 = 407.38 nM 6.39
CHEMBL456590 IC50 = 410.0 nM 6.39
CHEMBL456574 IC50 = 430.0 nM 6.37
CHEMBL456617 IC50 = 501.19 nM 6.30
CHEMBL63 ROLIPRAM IC50 = 549.54 nM 6.26
CHEMBL63 ROLIPRAM IC50 = 550.0 nM 6.26
CHEMBL458933 IC50 = 636.0 nM 6.20
CHEMBL458933 IC50 = 630.96 nM 6.20
CHEMBL45854 IC50 = 645.65 nM 6.19
CHEMBL458932 IC50 = 667.0 nM 6.18
CHEMBL458932 IC50 = 660.69 nM 6.18
CHEMBL443679 IC50 = 720.0 nM 6.14
CHEMBL443679 IC50 = 724.44 nM 6.14
CHEMBL456617 IC50 = 820.0 nM 6.09
CHEMBL457662 IC50 = 1096.48 nM 5.96
CHEMBL457662 IC50 = 1100.0 nM 5.96
CHEMBL298000 IC50 = 1584.89 nM 5.80
CHEMBL456327 IC50 = 1905.46 nM 5.72
CHEMBL456327 IC50 = 1900.0 nM 5.72
CHEMBL458931 IC50 = 2187.76 nM 5.66
CHEMBL458931 IC50 = 2200.0 nM 5.66
CHEMBL516301 IC50 = 2290.87 nM 5.64
CHEMBL460188 IC50 = 2570.4 nM 5.59
CHEMBL513099 IC50 = 2570.4 nM 5.59
CHEMBL513099 IC50 = 2600.0 nM 5.58
CHEMBL460188 IC50 = 2600.0 nM 5.58
CHEMBL44109 IC50 = 3090.3 nM 5.51
CHEMBL456368 IC50 = 3500.0 nM 5.46
CHEMBL456368 IC50 = 3467.37 nM 5.46