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Assay Detail

CHEMBL1805699

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Binding
Inhibition of PDE4D
21
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Discovery of MK-0952, a selective PDE4 inhibitor for the treatment of long-term memory loss and mild cognitive impairment.
Gallant M, Aspiotis R, Day S, Dias R, Dubé D, Dubé L, Friesen RW, Girard M, Guay D, Hamel P, Huang Z, Lacombe P, Laliberté S, Lévesque JF, Liu S, Macdonald D, Mancini J, Nicholson DW, Styhler A, Townson K, Waters K, Young RN, Girard Y.
Bioorg Med Chem Lett (2010) 20 : 6387 -6393
PubMed 20933411 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 8.97 9.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL253083 2 9.49
CHEMBL1801156 1 9.46
CHEMBL1801161 1 9.34
CHEMBL1801155 1 9.29
CHEMBL1801157 1 9.28
CHEMBL1801160 1 9.28
CHEMBL1801068 1 9.27
CHEMBL1801151 1 9.26
CHEMBL1801154 1 9.24
CHEMBL1801067 2 9.24
CHEMBL1801159 1 9.18
CHEMBL1801071 1 9.07
CHEMBL1801070 1 9.06
CHEMBL372575 1 9.00
CHEMBL1801158 1 9.00
CHEMBL1801069 1 8.34
CHEMBL485629 MK-0873 2.0 1 8.29
CHEMBL1801153 1 7.77
CHEMBL1801152 1 7.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL253083 IC50 = 0.32 nM 9.49
CHEMBL1801156 IC50 = 0.35 nM 9.46
CHEMBL1801161 IC50 = 0.46 nM 9.34
CHEMBL1801155 IC50 = 0.51 nM 9.29
CHEMBL1801160 IC50 = 0.53 nM 9.28
CHEMBL1801157 IC50 = 0.52 nM 9.28
CHEMBL253083 IC50 = 0.54 nM 9.27
CHEMBL1801068 IC50 = 0.54 nM 9.27
CHEMBL1801151 IC50 = 0.55 nM 9.26
CHEMBL1801067 IC50 = 0.57 nM 9.24
CHEMBL1801154 IC50 = 0.58 nM 9.24
CHEMBL1801159 IC50 = 0.66 nM 9.18
CHEMBL1801071 IC50 = 0.85 nM 9.07
CHEMBL1801070 IC50 = 0.88 nM 9.06
CHEMBL372575 IC50 = 1.0 nM 9.00
CHEMBL1801158 IC50 = 1.0 nM 9.00
CHEMBL1801067 IC50 = 1.6 nM 8.80
CHEMBL1801069 IC50 = 4.6 nM 8.34
CHEMBL485629 MK-0873 IC50 = 5.1 nM 8.29
CHEMBL1801153 IC50 = 17.0 nM 7.77
CHEMBL1801152 IC50 = 32.0 nM 7.50