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Assay Detail

CHEMBL828297

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

Binding
Inhibition of human Phosphodiesterase 7A1 or human phosphodiesterase 4D3 expressed in baculovirus infected Sf9 cells
ChEMBL ↗
34
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

Publication

Discovery of thiadiazoles as a novel structural class of potent and selective PDE7 inhibitors. Part 2: metabolism-directed optimization studies towards orally bioavailable derivatives.
Vergne F, Bernardelli P, Lorthiois E, Pham N, Proust E, Oliveira C, Mafroud AK, Ducrot P, Wrigglesworth R, Berlioz-Seux F, Coleon F, Chevalier E, Moreau F, Idrissi M, Tertre A, Descours A, Berna P, Li M.
Bioorg Med Chem Lett (2004) 14 : 4615 -4621
PubMed 15324875 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 5.72 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL185483 — — 4 7.30
CHEMBL363097 — — 2 7.22
CHEMBL185446 — — 2 7.22
CHEMBL183107 — — 8 7.10
CHEMBL360171 — — 2 7.10
CHEMBL425710 — — 2 6.92
CHEMBL182574 — — 2 6.80
CHEMBL363708 — — 2 6.72
CHEMBL362152 — — 2 6.72
CHEMBL185157 — — 2 6.42
CHEMBL363078 — — 2 6.38
CHEMBL184951 — — 4 6.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL185483 — IC50 = 50.0 nM 7.30
CHEMBL363097 — IC50 = 60.0 nM 7.22
CHEMBL185446 — IC50 = 60.0 nM 7.22
CHEMBL183107 — IC50 = 80.0 nM 7.10
CHEMBL360171 — IC50 = 80.0 nM 7.10
CHEMBL425710 — IC50 = 120.0 nM 6.92
CHEMBL182574 — IC50 = 160.0 nM 6.80
CHEMBL183107 — IC50 = 190.0 nM 6.72
CHEMBL363708 — IC50 = 190.0 nM 6.72
CHEMBL362152 — IC50 = 190.0 nM 6.72
CHEMBL185483 — IC50 = 310.0 nM 6.51
CHEMBL185157 — IC50 = 380.0 nM 6.42
CHEMBL363078 — IC50 = 420.0 nM 6.38
CHEMBL184951 — IC50 = 550.0 nM 6.26
CHEMBL184951 — IC50 = 610.0 nM 6.21
CHEMBL183107 — IC50 = 1650.0 nM 5.78
CHEMBL183107 — IC50 = 1740.0 nM 5.76
CHEMBL185446 — IC50 = 15300.0 nM 4.82
CHEMBL185483 — IC50 = 20000.0 nM 4.70
CHEMBL184951 — IC50 = 28500.0 nM 4.54
CHEMBL363097 — IC50 = 34250.0 nM 4.46
CHEMBL363708 — IC50 = 35670.0 nM 4.45
CHEMBL182574 — IC50 = 39660.0 nM 4.40
CHEMBL360171 — IC50 = 40800.0 nM 4.39
CHEMBL362152 — IC50 = 46330.0 nM 4.33
CHEMBL183107 — IC50 = 61620.0 nM 4.21
CHEMBL425710 — IC50 = 65500.0 nM 4.18
CHEMBL183107 — IC50 = 71640.0 nM 4.14
CHEMBL185483 — IC50 = 79170.0 nM 4.10
CHEMBL184951 — IC50 > 101000.0 nM -
CHEMBL183107 — IC50 > 101000.0 nM -
CHEMBL185157 — IC50 > 101000.0 nM -
CHEMBL363078 — IC50 > 101000.0 nM -
CHEMBL183107 — IC50 > 101000.0 nM -