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Assay Detail

CHEMBL3863951

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

Binding
Inhibition of PDE4 in PBMC (unknown origin) assessed as reduction in LPS-induced TNFalpha production incubated for 24 hrs by ELISA
ChEMBL ↗
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

Publication

Biphenyl Pyridazinone Derivatives as Inhaled PDE4 Inhibitors: Structural Biology and Structure-Activity Relationships.
Gràcia J, Buil MA, Castro J, Eichhorn P, Ferrer M, Gavaldà A, Hernández B, Segarra V, Lehner MD, Moreno I, Pagès L, Roberts RS, Serrat J, Sevilla S, Taltavull J, Andrés M, Cabedo J, Vilella D, Calama E, Carcasona C, Miralpeix M.
J Med Chem (2016) 59 : 10479 -10497
PubMed 27933955 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 44 9.13 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3913876 — — 1 10.30
CHEMBL3986586 — — 1 10.15
CHEMBL3958944 — — 1 10.05
CHEMBL3955694 — — 1 10.05
CHEMBL3918173 — — 1 9.72
CHEMBL3985784 — — 1 9.72
CHEMBL3925776 — — 1 9.70
CHEMBL3948448 — — 1 9.62
CHEMBL3968147 — — 1 9.62
CHEMBL3984510 — — 1 9.54
CHEMBL3903604 — — 1 9.54
CHEMBL3952586 — — 1 9.52
CHEMBL3945895 — — 1 9.52
CHEMBL3980193 — — 1 9.52
CHEMBL3919325 — — 1 9.51
CHEMBL3916846 — — 1 9.47
CHEMBL3922464 — — 1 9.46
CHEMBL3941862 — — 1 9.44
CHEMBL3977665 — — 1 9.40
CHEMBL3941513 — — 1 9.37
CHEMBL3905929 — — 1 9.28
CHEMBL3950249 — — 1 9.27
CHEMBL3984674 — — 1 9.26
CHEMBL3957127 — — 1 9.24
CHEMBL3892121 — — 1 9.17
CHEMBL3969954 — — 1 9.15
CHEMBL3966020 — — 1 9.10
CHEMBL3903408 — — 1 9.06
CHEMBL3950166 — — 1 9.06
CHEMBL3889823 — — 1 9.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3913876 — IC50 = 0.05 nM 10.30
CHEMBL3986586 — IC50 = 0.07 nM 10.15
CHEMBL3955694 — IC50 = 0.09 nM 10.05
CHEMBL3958944 — IC50 = 0.09 nM 10.05
CHEMBL3918173 — IC50 = 0.19 nM 9.72
CHEMBL3985784 — IC50 = 0.19 nM 9.72
CHEMBL3925776 — IC50 = 0.2 nM 9.70
CHEMBL3948448 — IC50 = 0.24 nM 9.62
CHEMBL3968147 — IC50 = 0.24 nM 9.62
CHEMBL3984510 — IC50 = 0.29 nM 9.54
CHEMBL3903604 — IC50 = 0.29 nM 9.54
CHEMBL3945895 — IC50 = 0.3 nM 9.52
CHEMBL3980193 — IC50 = 0.3 nM 9.52
CHEMBL3952586 — IC50 = 0.3 nM 9.52
CHEMBL3919325 — IC50 = 0.31 nM 9.51
CHEMBL3916846 — IC50 = 0.34 nM 9.47
CHEMBL3922464 — IC50 = 0.35 nM 9.46
CHEMBL3941862 — IC50 = 0.36 nM 9.44
CHEMBL3977665 — IC50 = 0.4 nM 9.40
CHEMBL3941513 — IC50 = 0.43 nM 9.37
CHEMBL3905929 — IC50 = 0.52 nM 9.28
CHEMBL3950249 — IC50 = 0.54 nM 9.27
CHEMBL3984674 — IC50 = 0.55 nM 9.26
CHEMBL3957127 — IC50 = 0.57 nM 9.24
CHEMBL3892121 — IC50 = 0.68 nM 9.17
CHEMBL3969954 — IC50 = 0.7 nM 9.15
CHEMBL3966020 — IC50 = 0.8 nM 9.10
CHEMBL3903408 — IC50 = 0.88 nM 9.06
CHEMBL3950166 — IC50 = 0.88 nM 9.06
CHEMBL3889823 — IC50 = 0.9 nM 9.05
CHEMBL3957296 — IC50 = 1.1 nM 8.96
CHEMBL3979212 — IC50 = 1.3 nM 8.89
CHEMBL3958869 — IC50 = 1.4 nM 8.85
CHEMBL3963331 — IC50 = 2.17 nM 8.66
CHEMBL3920544 — IC50 = 2.4 nM 8.62
CHEMBL3974515 — IC50 = 2.9 nM 8.54
CHEMBL3898745 — IC50 = 3.7 nM 8.43
CHEMBL193240 ROFLUMILAST IC50 = 4.0 nM 8.40
CHEMBL3896989 — IC50 = 4.9 nM 8.31
CHEMBL3931354 — IC50 = 6.6 nM 8.18
CHEMBL3912622 — IC50 = 10.3 nM 7.99
CHEMBL3935796 — IC50 = 11.6 nM 7.94
CHEMBL3978291 — IC50 = 21.0 nM 7.68
CHEMBL3909436 — IC50 = 26.3 nM 7.58