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Assay Detail

CHEMBL3744103

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Functional
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine receptor A2b (CHEMBL255)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

New substituted 9-propyladenine derivatives as A2Aadenosine receptor antagonists
Lambertucci C, Buccioni M, Dal Ben D, Kachler S, Marucci G, Spinaci A, Thomas A, Klotz K, Volpini R
Medchemcomm (2015) 6 : 963 -970
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 5.62 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL506450 1 6.70
CHEMBL3087706 1 6.60
CHEMBL3739795 1 5.83
CHEMBL475023 1 5.77
CHEMBL3740631 1 5.76
CHEMBL3741012 1 5.75
CHEMBL3739903 1 5.75
CHEMBL3742158 1 5.73
CHEMBL3740141 1 5.69
CHEMBL3740619 1 5.50
CHEMBL3741217 1 5.34
CHEMBL3739922 1 5.20
CHEMBL3741167 1 5.13
CHEMBL3740992 1 5.08
CHEMBL3739985 1 5.03
CHEMBL3741337 1 5.03
CHEMBL3741942 1 -
CHEMBL3739799 1 -
CHEMBL3742213 1 -
CHEMBL3739802 1 -
CHEMBL3740172 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL506450 Ki = 200.0 nM 6.70
CHEMBL3087706 Ki = 252.0 nM 6.60
CHEMBL3739795 Ki = 1490.0 nM 5.83
CHEMBL475023 Ki = 1700.0 nM 5.77
CHEMBL3740631 Ki = 1740.0 nM 5.76
CHEMBL3741012 Ki = 1760.0 nM 5.75
CHEMBL3739903 Ki = 1760.0 nM 5.75
CHEMBL3742158 Ki = 1870.0 nM 5.73
CHEMBL3740141 Ki = 2030.0 nM 5.69
CHEMBL3740619 Ki = 3190.0 nM 5.50
CHEMBL3741217 Ki = 4610.0 nM 5.34
CHEMBL3739922 Ki = 6300.0 nM 5.20
CHEMBL3741167 Ki = 7490.0 nM 5.13
CHEMBL3740992 Ki = 8240.0 nM 5.08
CHEMBL3739985 Ki = 9250.0 nM 5.03
CHEMBL3741337 Ki = 9280.0 nM 5.03
CHEMBL3741942 Ki > 30000.0 nM -
CHEMBL3739799 Ki > 30000.0 nM -
CHEMBL3742213 Ki > 30000.0 nM -
CHEMBL3739802 Ki > 30000.0 nM -
CHEMBL3740172 Ki > 30000.0 nM -