Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3119595

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

Binding
Inhibition of PDE4 activity in human PBMC assessed as inhibition of LPS-induced TNFalpha release after 18 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 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Phosphodiesterase 4 (CHEMBL2093863) ↗
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Novel class of benzoic acid ester derivatives as potent PDE4 inhibitors for inhaled administration in the treatment of respiratory diseases.
Armani E, Amari G, Rizzi A, De Fanti R, Ghidini E, Capaldi C, Carzaniga L, Caruso P, Guala M, Peretto I, La Porta E, Bolzoni PT, Facchinetti F, Carnini C, Moretto N, Patacchini R, Bassani F, Cenacchi V, Volta R, Amadei F, Capacchi S, Delcanale M, Puccini P, Catinella S, Civelli M, Villetti G.
J Med Chem (2014) 57 : 793 -816
PubMed 24400806 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 44 9.18 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3113943 — — 1 10.40
CHEMBL3113976 — — 1 10.22
CHEMBL3113974 TRANIMILAST 2.0 1 10.22
CHEMBL3113958 — — 1 9.96
CHEMBL3113975 — — 1 9.92
CHEMBL3113978 — — 1 9.92
CHEMBL3113977 — — 1 9.89
CHEMBL3113950 — — 1 9.89
CHEMBL3113960 — — 1 9.68
CHEMBL3113948 — — 1 9.60
CHEMBL3113964 — — 1 9.52
CHEMBL3113961 — — 1 9.47
CHEMBL3113951 — — 1 9.42
CHEMBL3113953 — — 1 9.39
CHEMBL3113955 — — 1 9.37
CHEMBL3113942 — — 1 9.33
CHEMBL3113965 — — 1 9.28
CHEMBL3113959 — — 1 9.20
CHEMBL3113939 — — 1 9.18
CHEMBL3113947 — — 1 9.17
CHEMBL3113963 — — 1 9.16
CHEMBL3113957 — — 1 9.16
CHEMBL3113945 — — 1 9.12
CHEMBL3113962 — — 1 9.07
CHEMBL3113968 — — 1 9.05
CHEMBL3113967 — — 1 9.04
CHEMBL3113946 — — 1 9.02
CHEMBL3113966 — — 1 9.02
CHEMBL3113952 — — 1 9.00
CHEMBL3113954 — — 1 8.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3113943 — IC50 = 0.04 nM 10.40
CHEMBL3113976 — IC50 = 0.06 nM 10.22
CHEMBL3113974 TRANIMILAST IC50 = 0.06 nM 10.22
CHEMBL3113958 — IC50 = 0.11 nM 9.96
CHEMBL3113975 — IC50 = 0.12 nM 9.92
CHEMBL3113978 — IC50 = 0.12 nM 9.92
CHEMBL3113977 — IC50 = 0.13 nM 9.89
CHEMBL3113950 — IC50 = 0.13 nM 9.89
CHEMBL3113960 — IC50 = 0.21 nM 9.68
CHEMBL3113948 — IC50 = 0.25 nM 9.60
CHEMBL3113964 — IC50 = 0.3 nM 9.52
CHEMBL3113961 — IC50 = 0.34 nM 9.47
CHEMBL3113951 — IC50 = 0.38 nM 9.42
CHEMBL3113953 — IC50 = 0.41 nM 9.39
CHEMBL3113955 — IC50 = 0.43 nM 9.37
CHEMBL3113942 — IC50 = 0.47 nM 9.33
CHEMBL3113965 — IC50 = 0.53 nM 9.28
CHEMBL3113959 — IC50 = 0.63 nM 9.20
CHEMBL3113939 — IC50 = 0.66 nM 9.18
CHEMBL3113947 — IC50 = 0.67 nM 9.17
CHEMBL3113963 — IC50 = 0.69 nM 9.16
CHEMBL3113957 — IC50 = 0.69 nM 9.16
CHEMBL3113945 — IC50 = 0.75 nM 9.12
CHEMBL3113962 — IC50 = 0.85 nM 9.07
CHEMBL3113968 — IC50 = 0.89 nM 9.05
CHEMBL3113967 — IC50 = 0.92 nM 9.04
CHEMBL3113946 — IC50 = 0.96 nM 9.02
CHEMBL3113966 — IC50 = 0.96 nM 9.02
CHEMBL3113952 — IC50 = 0.99 nM 9.00
CHEMBL3113954 — IC50 = 1.05 nM 8.98
CHEMBL3113936 — IC50 = 1.1 nM 8.96
CHEMBL3113970 — IC50 = 1.31 nM 8.88
CHEMBL3113944 — IC50 = 1.36 nM 8.87
CHEMBL3113937 — IC50 = 1.71 nM 8.77
CHEMBL3113949 — IC50 = 1.85 nM 8.73
CHEMBL3113938 — IC50 = 1.85 nM 8.73
CHEMBL3113956 — IC50 = 1.96 nM 8.71
CHEMBL3113941 — IC50 = 2.1 nM 8.68
CHEMBL3113969 — IC50 = 4.9 nM 8.31
CHEMBL3113940 — IC50 = 21.0 nM 7.68
CHEMBL3112603 — IC50 = 479.0 nM 6.32
CHEMBL3113971 — IC50 > 60.0 nM -
CHEMBL3113972 — IC50 > 60.0 nM -
CHEMBL3113973 — IC50 > 60.0 nM -