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Assay Detail

CHEMBL3744104

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

Binding
Displacement of [3H]HEMADO from human adenosine A3 receptor expressed in CHO cells
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Transmembrane domain-containing protein TMIGD3 (CHEMBL3712907)
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 5.71 7.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3741217 1 7.54
CHEMBL3740141 1 7.25
CHEMBL3740992 1 6.58
CHEMBL3739903 1 6.40
CHEMBL3740631 1 6.19
CHEMBL3087706 1 6.10
CHEMBL3741337 1 6.09
CHEMBL3742158 1 6.02
CHEMBL3739795 1 5.94
CHEMBL3739922 1 5.71
CHEMBL3740619 1 5.60
CHEMBL3739985 1 5.23
CHEMBL3740172 1 5.23
CHEMBL3741167 1 4.96
CHEMBL3741012 1 4.91
CHEMBL3741942 1 4.90
CHEMBL3742213 1 4.77
CHEMBL3739799 1 4.54
CHEMBL3739802 1 4.52
CHEMBL475023 1 -
CHEMBL506450 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3741217 Ki = 29.0 nM 7.54
CHEMBL3740141 Ki = 56.0 nM 7.25
CHEMBL3740992 Ki = 266.0 nM 6.58
CHEMBL3739903 Ki = 402.0 nM 6.40
CHEMBL3740631 Ki = 650.0 nM 6.19
CHEMBL3087706 Ki = 790.0 nM 6.10
CHEMBL3741337 Ki = 811.0 nM 6.09
CHEMBL3742158 Ki = 959.0 nM 6.02
CHEMBL3739795 Ki = 1160.0 nM 5.94
CHEMBL3739922 Ki = 1950.0 nM 5.71
CHEMBL3740619 Ki = 2520.0 nM 5.60
CHEMBL3739985 Ki = 5880.0 nM 5.23
CHEMBL3740172 Ki = 5840.0 nM 5.23
CHEMBL3741167 Ki = 11100.0 nM 4.96
CHEMBL3741012 Ki = 12200.0 nM 4.91
CHEMBL3741942 Ki = 12600.0 nM 4.90
CHEMBL3742213 Ki = 16900.0 nM 4.77
CHEMBL3739799 Ki = 29100.0 nM 4.54
CHEMBL3739802 Ki = 30000.0 nM 4.52
CHEMBL475023 Ki > 100000.0 nM -
CHEMBL506450 Ki > 100000.0 nM -