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Assay Detail

CHEMBL3748920

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Binding
Corrector activity at human CFTR F508 deletion mutant expressed in FRT cells incubated for 25 mins with forskolin by YFP-based fluorescence analysis relative to control
ChEMBL ↗
49
Total Activities
30
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type FRT
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cystic fibrosis transmembrane conductance regulator (CHEMBL4051) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel Hits in the Correction of ΔF508-Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Protein: Synthesis, Pharmacological, and ADME Evaluation of Tetrahydropyrido[4,3-d]pyrimidines for the Potential Treatment of Cystic Fibrosis.
Pesci E, Bettinetti L, Fanti P, Galietta LJ, La Rosa S, Magnoni L, Pedemonte N, Sardone GL, Maccari L.
J Med Chem (2015) 58 : 9697 -9711
PubMed 26561003 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Emax 30 - -
EC50 19 6.05 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3746133 — — 2 6.70
CHEMBL3745927 — — 2 6.70
CHEMBL3746547 — — 2 6.70
CHEMBL3747159 — — 2 6.70
CHEMBL3747771 — — 2 6.52
CHEMBL3746126 — — 2 6.52
CHEMBL3746769 — — 2 6.40
CHEMBL3745838 — — 2 6.16
CHEMBL3747604 — — 2 6.05
CHEMBL260775 — — 2 5.96
CHEMBL3746059 — — 2 5.85
CHEMBL3747046 — — 2 5.82
CHEMBL1257047 — — 2 5.66
CHEMBL3746321 — — 2 5.64
CHEMBL2103870 LUMACAFTOR 4.0 2 5.58
CHEMBL3745884 — — 2 5.55
CHEMBL3747654 — — 2 5.55
CHEMBL3746756 — — 2 5.51
CHEMBL3747330 — — 2 5.46
CHEMBL3745729 — — 1 -
CHEMBL3746219 — — 1 -
CHEMBL3745956 — — 1 -
CHEMBL3746375 — — 1 -
CHEMBL3745748 — — 1 -
CHEMBL3746313 — — 1 -
CHEMBL3746475 — — 1 -
CHEMBL3745870 — — 1 -
CHEMBL3746934 — — 1 -
CHEMBL3746584 — — 1 -
CHEMBL3747405 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3746547 — EC50 = 200.0 nM 6.70
CHEMBL3746133 — EC50 = 200.0 nM 6.70
CHEMBL3747159 — EC50 = 200.0 nM 6.70
CHEMBL3745927 — EC50 = 200.0 nM 6.70
CHEMBL3747771 — EC50 = 300.0 nM 6.52
CHEMBL3746126 — EC50 = 300.0 nM 6.52
CHEMBL3746769 — EC50 = 400.0 nM 6.40
CHEMBL3745838 — EC50 = 700.0 nM 6.16
CHEMBL3747604 — EC50 = 900.0 nM 6.05
CHEMBL260775 — EC50 = 1100.0 nM 5.96
CHEMBL3746059 — EC50 = 1400.0 nM 5.85
CHEMBL3747046 — EC50 = 1500.0 nM 5.82
CHEMBL1257047 — EC50 = 2200.0 nM 5.66
CHEMBL3746321 — EC50 = 2300.0 nM 5.64
CHEMBL2103870 LUMACAFTOR EC50 = 2600.0 nM 5.58
CHEMBL3745884 — EC50 = 2800.0 nM 5.55
CHEMBL3747654 — EC50 = 2800.0 nM 5.55
CHEMBL3746756 — EC50 = 3100.0 nM 5.51
CHEMBL3747330 — EC50 = 3500.0 nM 5.46
CHEMBL3745748 — Emax - — -
CHEMBL2103870 LUMACAFTOR Emax = 66.7 % -
CHEMBL1257047 — Emax = 92.9 % -
CHEMBL260775 — Emax = 113.8 % -
CHEMBL3747654 — Emax = 57.9 % -
CHEMBL3746059 — Emax = 56.6 % -
CHEMBL3745884 — Emax = 62.9 % -
CHEMBL3745729 — Emax - — -
CHEMBL3746313 — Emax - — -
CHEMBL3746475 — Emax - — -
CHEMBL3745870 — Emax - — -
CHEMBL3746934 — Emax - — -
CHEMBL3746584 — Emax - — -
CHEMBL3746375 — Emax - — -
CHEMBL3746219 — Emax - — -
CHEMBL3747604 — Emax = 41.0 % -
CHEMBL3747771 — Emax = 57.2 % -
CHEMBL3746133 — Emax = 79.8 % -
CHEMBL3747159 — Emax = 40.0 % -
CHEMBL3745927 — Emax = 73.8 % -
CHEMBL3745838 — Emax = 65.6 % -
CHEMBL3746126 — Emax = 36.9 % -
CHEMBL3747405 — Emax - — -
CHEMBL3746547 — Emax = 40.6 % -
CHEMBL3747330 — Emax = 86.6 % -
CHEMBL3746769 — Emax = 106.9 % -
CHEMBL3747046 — Emax = 41.3 % -
CHEMBL3746756 — Emax = 53.4 % -
CHEMBL3745956 — Emax - — -
CHEMBL3746321 — Emax = 35.9 % -