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Assay Detail

CHEMBL646606

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

Binding
Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in HEK 293 cells
ChEMBL ↗
43
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Adenosine receptor A3 (CHEMBL256) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Thiazole and thiadiazole analogues as a novel class of adenosine receptor antagonists.
van Muijlwijk-Koezen JE, Timmerman H, Vollinga RC, Frijtag von Drabbe Künzel J, de Groote M, Visser S, IJzerman AP.
J Med Chem (2001) 44 : 749 -762
PubMed 11262085 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 43 6.07 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL70880 — — 1 8.40
CHEMBL128929 — — 1 7.77
CHEMBL167627 — — 1 7.57
CHEMBL62075 — — 1 7.10
CHEMBL305322 — — 1 7.09
CHEMBL273094 XANTHINE AMINE CONGENER — 1 6.96
CHEMBL164745 — — 1 6.89
CHEMBL16687 CGS-15943 — 1 6.85
CHEMBL353651 — — 1 6.85
CHEMBL52735 — — 1 6.77
CHEMBL71053 — — 1 6.70
CHEMBL424259 — — 1 6.64
CHEMBL435866 — — 1 6.62
CHEMBL165783 — — 1 6.39
CHEMBL165741 — — 1 6.28
CHEMBL165103 — — 1 6.24
CHEMBL60156 — — 1 6.17
CHEMBL162000 — — 1 6.10
CHEMBL353126 — — 1 5.96
CHEMBL354004 — — 1 5.92
CHEMBL163248 — — 1 5.92
CHEMBL165971 — — 2 5.77
CHEMBL165784 — — 1 5.75
CHEMBL167985 — — 2 5.72
CHEMBL162808 — — 1 5.68
CHEMBL349715 — — 1 5.60
CHEMBL352267 — — 1 5.55
CHEMBL348973 — — 1 5.50
CHEMBL351051 — — 1 5.50
CHEMBL162990 — — 1 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL70880 — Ki = 4.0 nM 8.40
CHEMBL128929 — Ki = 17.0 nM 7.77
CHEMBL167627 — Ki = 27.0 nM 7.57
CHEMBL62075 — Ki = 79.0 nM 7.10
CHEMBL305322 — Ki = 82.0 nM 7.09
CHEMBL273094 XANTHINE AMINE CONGENER Ki = 110.0 nM 6.96
CHEMBL164745 — Ki = 130.0 nM 6.89
CHEMBL16687 CGS-15943 Ki = 140.0 nM 6.85
CHEMBL353651 — Ki = 140.0 nM 6.85
CHEMBL52735 — Ki = 170.0 nM 6.77
CHEMBL71053 — Ki = 200.0 nM 6.70
CHEMBL424259 — Ki = 230.0 nM 6.64
CHEMBL435866 — Ki = 240.0 nM 6.62
CHEMBL165783 — Ki = 410.0 nM 6.39
CHEMBL165741 — Ki = 520.0 nM 6.28
CHEMBL165103 — Ki = 580.0 nM 6.24
CHEMBL60156 — Ki = 670.0 nM 6.17
CHEMBL162000 — Ki = 800.0 nM 6.10
CHEMBL353126 — Ki = 1100.0 nM 5.96
CHEMBL354004 — Ki = 1200.0 nM 5.92
CHEMBL163248 — Ki = 1200.0 nM 5.92
CHEMBL165971 — Ki = 1700.0 nM 5.77
CHEMBL165784 — Ki = 1800.0 nM 5.75
CHEMBL167985 — Ki = 1900.0 nM 5.72
CHEMBL162808 — Ki = 2100.0 nM 5.68
CHEMBL349715 — Ki = 2500.0 nM 5.60
CHEMBL167985 — Ki = 2700.0 nM 5.57
CHEMBL352267 — Ki = 2800.0 nM 5.55
CHEMBL348973 — Ki = 3200.0 nM 5.50
CHEMBL351051 — Ki = 3200.0 nM 5.50
CHEMBL162990 — Ki = 3300.0 nM 5.48
CHEMBL164087 — Ki = 3400.0 nM 5.47
CHEMBL162033 — Ki = 3500.0 nM 5.46
CHEMBL161981 — Ki = 3700.0 nM 5.43
CHEMBL167391 — Ki = 4000.0 nM 5.40
CHEMBL163040 — Ki = 4600.0 nM 5.34
CHEMBL164422 — Ki = 5000.0 nM 5.30
CHEMBL165971 — Ki = 5300.0 nM 5.28
CHEMBL164276 — Ki = 8700.0 nM 5.06
CHEMBL355832 — Ki = 9900.0 nM 5.00
CHEMBL164783 — Ki = 10000.0 nM 5.00
CHEMBL164782 — Ki = 16000.0 nM 4.80
CHEMBL162271 — Ki = 147000.0 nM -