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Assay Detail

CHEMBL757136

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

Binding
Inhibition of phosphodiesterase type 4 isozyme (PDE4) from the U937 human cell line.
ChEMBL ↗
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type U-937
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

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

Publication

Synthesis, structure-activity relationships, and pharmacological profile of 9-amino-4-oxo-1-phenyl-3,4,6,7-tetrahydro[1,4]diazepino[6, 7,1-hi]indoles: discovery of potent, selective phosphodiesterase type 4 inhibitors.
Burnouf C, Auclair E, Avenel N, Bertin B, Bigot C, Calvet A, Chan K, Durand C, Fasquelle V, Féru F, Gilbertsen R, Jacobelli H, Kebsi A, Lallier E, Maignel J, Martin B, Milano S, Ouagued M, Pascal Y, Pruniaux MP, Puaud J, Rocher MN, Terrasse C, Wrigglesworth R, Doherty AM.
J Med Chem (2000) 43 : 4850 -4867
PubMed 11123995 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 6.10 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL511115 CILOMILAST 3.0 1 7.52
CHEMBL146218 — — 1 7.40
CHEMBL145390 — — 1 7.10
CHEMBL145499 — — 1 7.05
CHEMBL145258 — — 1 7.00
CHEMBL144287 — — 1 6.70
CHEMBL144245 — — 1 6.70
CHEMBL144258 — — 1 6.70
CHEMBL422653 — — 1 6.70
CHEMBL144404 — — 1 6.70
CHEMBL342285 — — 1 6.57
CHEMBL125671 — — 1 6.52
CHEMBL423931 — — 1 6.52
CHEMBL434516 — — 1 6.30
CHEMBL112366 — — 1 6.30
CHEMBL357197 — — 1 6.16
CHEMBL125123 — — 1 6.16
CHEMBL144570 — — 1 6.16
CHEMBL343243 — — 1 6.16
CHEMBL63 ROLIPRAM 2.0 1 6.03
CHEMBL341671 — — 1 6.00
CHEMBL111925 — — 1 5.96
CHEMBL339749 — — 1 5.89
CHEMBL341662 — — 1 5.85
CHEMBL126581 — — 1 5.80
CHEMBL434838 — — 1 5.77
CHEMBL339408 — — 1 5.58
CHEMBL436207 — — 1 5.57
CHEMBL418848 — — 1 5.36
CHEMBL422828 — — 1 5.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL511115 CILOMILAST IC50 = 30.0 nM 7.52
CHEMBL146218 — IC50 = 40.0 nM 7.40
CHEMBL145390 — IC50 = 80.0 nM 7.10
CHEMBL145499 — IC50 = 90.0 nM 7.05
CHEMBL145258 — IC50 = 100.0 nM 7.00
CHEMBL144287 — IC50 = 200.0 nM 6.70
CHEMBL144245 — IC50 = 200.0 nM 6.70
CHEMBL144258 — IC50 = 200.0 nM 6.70
CHEMBL422653 — IC50 = 200.0 nM 6.70
CHEMBL144404 — IC50 = 200.0 nM 6.70
CHEMBL342285 — IC50 = 270.0 nM 6.57
CHEMBL125671 — IC50 = 300.0 nM 6.52
CHEMBL423931 — IC50 = 300.0 nM 6.52
CHEMBL434516 — IC50 = 500.0 nM 6.30
CHEMBL112366 — IC50 = 500.0 nM 6.30
CHEMBL125123 — IC50 = 700.0 nM 6.16
CHEMBL144570 — IC50 = 690.0 nM 6.16
CHEMBL357197 — IC50 = 700.0 nM 6.16
CHEMBL343243 — IC50 = 700.0 nM 6.16
CHEMBL63 ROLIPRAM IC50 = 930.0 nM 6.03
CHEMBL341671 — IC50 = 1000.0 nM 6.00
CHEMBL111925 — IC50 = 1100.0 nM 5.96
CHEMBL339749 — IC50 = 1300.0 nM 5.89
CHEMBL341662 — IC50 = 1400.0 nM 5.85
CHEMBL126581 — IC50 = 1600.0 nM 5.80
CHEMBL434838 — IC50 = 1700.0 nM 5.77
CHEMBL339408 — IC50 = 2600.0 nM 5.58
CHEMBL436207 — IC50 = 2700.0 nM 5.57
CHEMBL418848 — IC50 = 4400.0 nM 5.36
CHEMBL422828 — IC50 = 4700.0 nM 5.33
CHEMBL125828 — IC50 = 5500.0 nM 5.26
CHEMBL357616 — IC50 = 6200.0 nM 5.21
CHEMBL144370 — IC50 = 10500.0 nM 4.98
CHEMBL144452 — IC50 = 10800.0 nM 4.97
CHEMBL356548 — IC50 = 16200.0 nM 4.79
CHEMBL144605 — IC50 = 20500.0 nM 4.69
CHEMBL344726 — IC50 > 100000.0 nM -