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Assay Detail

CHEMBL3374135

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

Binding
Inhibition of PDE7A (unknown origin)
22
Total Activities
22
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

High affinity 3',5'-cyclic-AMP phosphodiesterase 7A (CHEMBL3012)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and SAR study of 2-(4-pyridylamino)thieno[3,2-d]pyrimidin-4(3H)-ones as soluble and highly potent PDE7 inhibitors.
Endo Y, Kawai K, Asano T, Amano S, Asanuma Y, Sawada K, Ogura K, Nagata N, Ueo N, Takahashi N, Sonoda Y, Kamei N.
Bioorg Med Chem Lett (2015) 25 : 649 -653
PubMed 25529739 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 7.72 9.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3360172 1 9.49
CHEMBL3360170 1 9.17
CHEMBL3360169 1 8.96
CHEMBL3360171 1 8.92
CHEMBL3354179 1 8.70
CHEMBL3360167 1 8.68
CHEMBL3360168 1 8.41
CHEMBL3360166 1 8.06
CHEMBL3360165 1 7.60
CHEMBL3360161 1 7.39
CHEMBL3360164 1 7.22
CHEMBL3360160 1 7.21
CHEMBL3360155 1 7.06
CHEMBL3354160 1 6.82
CHEMBL3354155 1 6.80
CHEMBL3360154 1 6.54
CHEMBL3360163 1 6.20
CHEMBL3360159 1 5.64
CHEMBL3360162 1 -
CHEMBL3360158 1 -
CHEMBL3360157 1 -
CHEMBL3360156 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3360172 IC50 = 0.32 nM 9.49
CHEMBL3360170 IC50 = 0.68 nM 9.17
CHEMBL3360169 IC50 = 1.1 nM 8.96
CHEMBL3360171 IC50 = 1.2 nM 8.92
CHEMBL3354179 IC50 = 2.0 nM 8.70
CHEMBL3360167 IC50 = 2.1 nM 8.68
CHEMBL3360168 IC50 = 3.9 nM 8.41
CHEMBL3360166 IC50 = 8.7 nM 8.06
CHEMBL3360165 IC50 = 25.0 nM 7.60
CHEMBL3360161 IC50 = 41.0 nM 7.39
CHEMBL3360164 IC50 = 60.0 nM 7.22
CHEMBL3360160 IC50 = 61.0 nM 7.21
CHEMBL3360155 IC50 = 88.0 nM 7.06
CHEMBL3354160 IC50 = 150.0 nM 6.82
CHEMBL3354155 IC50 = 160.0 nM 6.80
CHEMBL3360154 IC50 = 290.0 nM 6.54
CHEMBL3360163 IC50 = 630.0 nM 6.20
CHEMBL3360159 IC50 = 2300.0 nM 5.64
CHEMBL3360162 IC50 > 1000.0 nM -
CHEMBL3360158 IC50 > 1000.0 nM -
CHEMBL3360157 IC50 > 1000.0 nM -
CHEMBL3360156 IC50 > 1000.0 nM -