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Assay Detail

CHEMBL3119596

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Binding
Inhibition of PDE4 isolated from human U937 cells assessed as reduction in cAMP level by LANCE assay
ChEMBL ↗
54
Total Activities
54
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type U-937
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 54 9.65 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3113949 — — 1 10.52
CHEMBL3113948 — — 1 10.52
CHEMBL3113966 — — 1 10.52
CHEMBL3113954 — — 1 10.52
CHEMBL3113976 — — 1 10.40
CHEMBL3113974 TRANIMILAST 2.0 1 10.40
CHEMBL3113968 — — 1 10.40
CHEMBL3113962 — — 1 10.40
CHEMBL3113950 — — 1 10.30
CHEMBL3113953 — — 1 10.30
CHEMBL3113943 — — 1 10.30
CHEMBL3113946 — — 1 10.30
CHEMBL3113964 — — 1 10.30
CHEMBL3113967 — — 1 10.22
CHEMBL3113955 — — 1 10.22
CHEMBL3113951 — — 1 10.22
CHEMBL3113978 — — 1 10.15
CHEMBL3113937 — — 1 10.14
CHEMBL3113963 — — 1 10.10
CHEMBL3113945 — — 1 10.10
CHEMBL3113947 — — 1 10.10
CHEMBL3113958 — — 1 10.05
CHEMBL3113939 — — 1 10.00
CHEMBL3113975 — — 1 9.89
CHEMBL3113942 — — 1 9.85
CHEMBL3113961 — — 1 9.82
CHEMBL3113938 — — 1 9.80
CHEMBL3113977 — — 1 9.77
CHEMBL3113970 — — 1 9.74
CHEMBL3113940 — — 1 9.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3113949 — IC50 = 0.03 nM 10.52
CHEMBL3113954 — IC50 = 0.03 nM 10.52
CHEMBL3113966 — IC50 = 0.03 nM 10.52
CHEMBL3113948 — IC50 = 0.03 nM 10.52
CHEMBL3113976 — IC50 = 0.04 nM 10.40
CHEMBL3113974 TRANIMILAST IC50 = 0.04 nM 10.40
CHEMBL3113968 — IC50 = 0.04 nM 10.40
CHEMBL3113962 — IC50 = 0.04 nM 10.40
CHEMBL3113950 — IC50 = 0.05 nM 10.30
CHEMBL3113953 — IC50 = 0.05 nM 10.30
CHEMBL3113943 — IC50 = 0.05 nM 10.30
CHEMBL3113946 — IC50 = 0.05 nM 10.30
CHEMBL3113964 — IC50 = 0.05 nM 10.30
CHEMBL3113955 — IC50 = 0.06 nM 10.22
CHEMBL3113967 — IC50 = 0.06 nM 10.22
CHEMBL3113951 — IC50 = 0.06 nM 10.22
CHEMBL3113978 — IC50 = 0.07 nM 10.15
CHEMBL3113937 — IC50 = 0.072 nM 10.14
CHEMBL3113963 — IC50 = 0.08 nM 10.10
CHEMBL3113945 — IC50 = 0.08 nM 10.10
CHEMBL3113947 — IC50 = 0.08 nM 10.10
CHEMBL3113958 — IC50 = 0.09 nM 10.05
CHEMBL3113939 — IC50 = 0.1 nM 10.00
CHEMBL3113975 — IC50 = 0.13 nM 9.89
CHEMBL3113942 — IC50 = 0.14 nM 9.85
CHEMBL3113961 — IC50 = 0.15 nM 9.82
CHEMBL3113938 — IC50 = 0.16 nM 9.80
CHEMBL3113977 — IC50 = 0.17 nM 9.77
CHEMBL3113970 — IC50 = 0.18 nM 9.74
CHEMBL3113940 — IC50 = 0.2 nM 9.70
CHEMBL3113957 — IC50 = 0.21 nM 9.68
CHEMBL3113944 — IC50 = 0.21 nM 9.68
CHEMBL3113936 — IC50 = 0.22 nM 9.66
CHEMBL3113960 — IC50 = 0.24 nM 9.62
CHEMBL3113956 — IC50 = 0.26 nM 9.59
CHEMBL3113959 — IC50 = 0.31 nM 9.51
CHEMBL3113965 — IC50 = 0.32 nM 9.49
CHEMBL3113972 — IC50 = 0.4 nM 9.40
CHEMBL3113969 — IC50 = 0.4 nM 9.40
CHEMBL3113941 — IC50 = 0.41 nM 9.39
CHEMBL3113952 — IC50 = 0.56 nM 9.25
CHEMBL3113971 — IC50 = 0.73 nM 9.14
CHEMBL3113931 — IC50 = 1.06 nM 8.97
CHEMBL3113932 — IC50 = 1.14 nM 8.94
CHEMBL3113736 — IC50 = 1.18 nM 8.93
CHEMBL3113930 — IC50 = 1.34 nM 8.87
CHEMBL3113929 — IC50 = 1.74 nM 8.76
CHEMBL3113934 — IC50 = 1.9 nM 8.72
CHEMBL3113935 — IC50 = 2.43 nM 8.61
CHEMBL3113737 — IC50 = 3.45 nM 8.46