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Assay Detail

CHEMBL1021383

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

Binding
Displacement of radioligand from human recombinant adenosine A1 receptor at 21 degC after 90 mins by cell-based microplate scintillation counting
ChEMBL ↗
58
Total Activities
58
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine receptor A1 (CHEMBL226) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines.
Gillespie RJ, Bamford SJ, Botting R, Comer M, Denny S, Gaur S, Griffin M, Jordan AM, Knight AR, Lerpiniere J, Leonardi S, Lightowler S, McAteer S, Merrett A, Misra A, Padfield A, Reece M, Saadi M, Selwood DL, Stratton GC, Surry D, Todd R, Tong X, Ruston V, Upton R, Weiss SM.
J Med Chem (2009) 52 : 33 -47
PubMed 19072055 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 58 6.59 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL461857 — — 1 7.72
CHEMBL518364 — — 1 7.58
CHEMBL468256 — — 1 7.57
CHEMBL510134 — — 1 7.40
CHEMBL467246 — — 1 7.38
CHEMBL461651 — — 1 7.35
CHEMBL459322 — — 1 7.30
CHEMBL516483 — — 1 7.20
CHEMBL447664 VIPADENANT 2.0 1 7.17
CHEMBL462488 — — 1 7.12
CHEMBL518497 — — 1 7.11
CHEMBL461650 — — 1 7.11
CHEMBL506101 — — 1 7.11
CHEMBL507426 — — 1 7.08
CHEMBL449469 — — 1 7.07
CHEMBL467245 — — 1 7.01
CHEMBL461649 — — 1 7.00
CHEMBL517278 — — 1 6.98
CHEMBL517429 — — 1 6.98
CHEMBL467244 — — 1 6.96
CHEMBL460799 — — 1 6.93
CHEMBL513661 — — 1 6.93
CHEMBL517886 — — 1 6.92
CHEMBL517417 — — 1 6.88
CHEMBL461008 — — 1 6.88
CHEMBL511405 — — 1 6.81
CHEMBL516611 — — 1 6.74
CHEMBL516800 — — 1 6.72
CHEMBL460975 — — 1 6.72
CHEMBL512812 — — 1 6.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL461857 — Ki = 19.0 nM 7.72
CHEMBL518364 — Ki = 26.0 nM 7.58
CHEMBL468256 — Ki = 27.0 nM 7.57
CHEMBL510134 — Ki = 40.0 nM 7.40
CHEMBL467246 — Ki = 42.0 nM 7.38
CHEMBL461651 — Ki = 45.0 nM 7.35
CHEMBL459322 — Ki = 50.0 nM 7.30
CHEMBL516483 — Ki = 63.0 nM 7.20
CHEMBL447664 VIPADENANT Ki = 68.0 nM 7.17
CHEMBL462488 — Ki = 76.0 nM 7.12
CHEMBL518497 — Ki = 77.0 nM 7.11
CHEMBL461650 — Ki = 77.0 nM 7.11
CHEMBL506101 — Ki = 78.0 nM 7.11
CHEMBL507426 — Ki = 83.0 nM 7.08
CHEMBL449469 — Ki = 86.0 nM 7.07
CHEMBL467245 — Ki = 98.0 nM 7.01
CHEMBL461649 — Ki = 100.0 nM 7.00
CHEMBL517278 — Ki = 105.0 nM 6.98
CHEMBL517429 — Ki = 105.0 nM 6.98
CHEMBL467244 — Ki = 110.0 nM 6.96
CHEMBL460799 — Ki = 117.0 nM 6.93
CHEMBL513661 — Ki = 118.0 nM 6.93
CHEMBL517886 — Ki = 120.0 nM 6.92
CHEMBL517417 — Ki = 132.0 nM 6.88
CHEMBL461008 — Ki = 131.0 nM 6.88
CHEMBL511405 — Ki = 154.0 nM 6.81
CHEMBL516611 — Ki = 183.0 nM 6.74
CHEMBL516800 — Ki = 190.0 nM 6.72
CHEMBL460975 — Ki = 190.0 nM 6.72
CHEMBL512812 — Ki = 190.0 nM 6.72
CHEMBL505787 — Ki = 203.0 nM 6.69
CHEMBL467035 — Ki = 230.0 nM 6.64
CHEMBL508451 — Ki = 231.0 nM 6.64
CHEMBL516770 — Ki = 249.0 nM 6.60
CHEMBL442670 — Ki = 291.0 nM 6.54
CHEMBL506511 — Ki = 314.0 nM 6.50
CHEMBL443665 — Ki = 319.0 nM 6.50
CHEMBL517418 — Ki = 400.0 nM 6.40
CHEMBL508558 — Ki = 553.0 nM 6.26
CHEMBL468701 — Ki = 599.0 nM 6.22
CHEMBL260557 — Ki = 647.0 nM 6.19
CHEMBL518178 — Ki = 700.0 nM 6.16
CHEMBL461007 — Ki = 738.0 nM 6.13
CHEMBL460596 — Ki = 733.0 nM 6.13
CHEMBL505977 — Ki = 769.0 nM 6.11
CHEMBL467867 — Ki = 894.0 nM 6.05
CHEMBL449596 — Ki = 931.0 nM 6.03
CHEMBL462501 — Ki = 1117.0 nM 5.95
CHEMBL460805 — Ki = 1133.0 nM 5.95
CHEMBL517277 — Ki = 1166.0 nM 5.93