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Assay Detail

CHEMBL824111

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

Binding
Inhibition of cyclic AMP-phosphodiesterase ( PDE) in the supernatant of tracheal muscle homogenate
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Muscle tissue
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Phosphodiesterase 4 (CHEMBL2093863)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Bronchodilator activity of xanthine derivatives substituted with functional groups at the 1- or 7-position.
Miyamoto K, Yamamoto Y, Kurita M, Sakai R, Konno K, Sanae F, Ohshima T, Takagi K, Hasegawa T, Iwasaki N.
J Med Chem (1993) 36 : 1380 -1386
PubMed 8496906 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 42 4.54 5.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL29272 1 5.09
CHEMBL32184 1 5.05
CHEMBL286976 1 4.97
CHEMBL283454 1 4.90
CHEMBL282394 1 4.89
CHEMBL27967 1 4.85
CHEMBL29518 1 4.84
CHEMBL28559 1 4.79
CHEMBL28879 1 4.78
CHEMBL27969 1 4.68
CHEMBL28075 1 4.65
CHEMBL28194 1 4.62
CHEMBL288786 1 4.62
CHEMBL157655 1 4.58
CHEMBL28300 1 4.58
CHEMBL29461 1 4.56
CHEMBL283020 1 4.54
CHEMBL28980 1 4.52
CHEMBL282310 1 4.51
CHEMBL283412 1 4.49
CHEMBL31859 1 4.48
CHEMBL287180 1 4.45
CHEMBL628 PENTOXIFYLLINE 4.0 1 4.42
CHEMBL32241 1 4.39
CHEMBL279898 ENPROFYLLINE 2.0 1 4.37
CHEMBL28683 1 4.34
CHEMBL28603 1 4.33
CHEMBL445847 1 4.31
CHEMBL286741 1 4.28
CHEMBL1355736 THEOPHYLLINE 4.0 1 4.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL29272 Ki = 8200.0 nM 5.09
CHEMBL32184 Ki = 9000.0 nM 5.05
CHEMBL286976 Ki = 10600.0 nM 4.97
CHEMBL283454 Ki = 12600.0 nM 4.90
CHEMBL282394 Ki = 13000.0 nM 4.89
CHEMBL27967 Ki = 14100.0 nM 4.85
CHEMBL29518 Ki = 14600.0 nM 4.84
CHEMBL28559 Ki = 16400.0 nM 4.79
CHEMBL28879 Ki = 16500.0 nM 4.78
CHEMBL27969 Ki = 20700.0 nM 4.68
CHEMBL28075 Ki = 22300.0 nM 4.65
CHEMBL288786 Ki = 23800.0 nM 4.62
CHEMBL28194 Ki = 24100.0 nM 4.62
CHEMBL157655 Ki = 26100.0 nM 4.58
CHEMBL28300 Ki = 26200.0 nM 4.58
CHEMBL29461 Ki = 27300.0 nM 4.56
CHEMBL283020 Ki = 28700.0 nM 4.54
CHEMBL28980 Ki = 29900.0 nM 4.52
CHEMBL282310 Ki = 30800.0 nM 4.51
CHEMBL283412 Ki = 32300.0 nM 4.49
CHEMBL31859 Ki = 32800.0 nM 4.48
CHEMBL287180 Ki = 35800.0 nM 4.45
CHEMBL628 PENTOXIFYLLINE Ki = 37700.0 nM 4.42
CHEMBL32241 Ki = 40800.0 nM 4.39
CHEMBL279898 ENPROFYLLINE Ki = 43100.0 nM 4.37
CHEMBL28683 Ki = 46000.0 nM 4.34
CHEMBL28603 Ki = 46400.0 nM 4.33
CHEMBL445847 Ki = 48700.0 nM 4.31
CHEMBL286741 Ki = 53000.0 nM 4.28
CHEMBL1355736 THEOPHYLLINE Ki = 56800.0 nM 4.25
CHEMBL31838 Ki = 56300.0 nM 4.25
CHEMBL28419 Ki = 60000.0 nM 4.22
CHEMBL28298 Ki = 72700.0 nM 4.14
CHEMBL282160 Ki = 92000.0 nM 4.04
CHEMBL28684 Ki = 92400.0 nM 4.03
CHEMBL28295 Ki > 200000.0 nM -
CHEMBL281972 Ki = 119000.0 nM -
CHEMBL29052 Ki > 200000.0 nM -
CHEMBL29209 Ki > 200000.0 nM -
CHEMBL27970 Ki > 200000.0 nM -
CHEMBL27915 Ki > 200000.0 nM -
CHEMBL283024 Ki = 136000.0 nM -