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Assay Detail

CHEMBL680424

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Functional
Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Adenosine receptor A2a (CHEMBL251)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Effects of alkyl substitutions of xanthine skeleton on bronchodilation.
Sakai R, Konno K, Yamamoto Y, Sanae F, Takagi K, Hasegawa T, Iwasaki N, Kakiuchi M, Kato H, Miyamoto K.
J Med Chem (1992) 35 : 4039 -4044
PubMed 1331453 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 30 5.21 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL446679 1 7.52
CHEMBL157655 1 7.30
CHEMBL278332 1 6.22
CHEMBL28194 1 5.89
CHEMBL130969 1 5.89
CHEMBL132001 1 5.85
CHEMBL286976 1 5.80
CHEMBL131275 1 5.51
CHEMBL334813 1 5.33
CHEMBL282310 1 5.30
CHEMBL283412 1 5.23
CHEMBL279898 ENPROFYLLINE 2.0 1 5.14
CHEMBL130503 1 5.12
CHEMBL132052 1 5.12
CHEMBL337001 1 5.08
CHEMBL334849 1 5.08
CHEMBL112369 1 5.02
CHEMBL417654 1 4.97
CHEMBL131164 1 4.86
CHEMBL24107 1 4.82
CHEMBL128900 1 4.81
CHEMBL131371 1 4.56
CHEMBL1355736 THEOPHYLLINE 4.0 1 4.55
CHEMBL68278 1 4.36
CHEMBL39986 1 4.21
CHEMBL131181 1 4.16
CHEMBL1250 1-METHYLXANTHINE 1 4.12
CHEMBL127167 1 4.02
CHEMBL1424 XANTHINE 1 -
CHEMBL619 3-METHYLXANTHINE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL446679 EC50 = 30.0 nM 7.52
CHEMBL157655 EC50 = 50.0 nM 7.30
CHEMBL278332 EC50 = 600.0 nM 6.22
CHEMBL28194 EC50 = 1300.0 nM 5.89
CHEMBL130969 EC50 = 1300.0 nM 5.89
CHEMBL132001 EC50 = 1400.0 nM 5.85
CHEMBL286976 EC50 = 1600.0 nM 5.80
CHEMBL131275 EC50 = 3100.0 nM 5.51
CHEMBL334813 EC50 = 4700.0 nM 5.33
CHEMBL282310 EC50 = 5000.0 nM 5.30
CHEMBL283412 EC50 = 5900.0 nM 5.23
CHEMBL279898 ENPROFYLLINE EC50 = 7200.0 nM 5.14
CHEMBL130503 EC50 = 7600.0 nM 5.12
CHEMBL132052 EC50 = 7600.0 nM 5.12
CHEMBL337001 EC50 = 8300.0 nM 5.08
CHEMBL334849 EC50 = 8300.0 nM 5.08
CHEMBL112369 EC50 = 9600.0 nM 5.02
CHEMBL417654 EC50 = 10600.0 nM 4.97
CHEMBL131164 EC50 = 13800.0 nM 4.86
CHEMBL24107 EC50 = 15200.0 nM 4.82
CHEMBL128900 EC50 = 15500.0 nM 4.81
CHEMBL131371 EC50 = 27500.0 nM 4.56
CHEMBL1355736 THEOPHYLLINE EC50 = 28200.0 nM 4.55
CHEMBL68278 EC50 = 43400.0 nM 4.36
CHEMBL39986 EC50 = 62000.0 nM 4.21
CHEMBL131181 EC50 = 69200.0 nM 4.16
CHEMBL1250 1-METHYLXANTHINE EC50 = 75900.0 nM 4.12
CHEMBL127167 EC50 = 96200.0 nM 4.02
CHEMBL1424 XANTHINE EC50 > 100000.0 nM -
CHEMBL619 3-METHYLXANTHINE EC50 > 100000.0 nM -