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Assay Detail

CHEMBL921474

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

Binding
Binding affinity at human adenosine A1 receptor
ChEMBL ↗
67
Total Activities
67
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 adenosine A2A receptor. Part 3: Design and synthesis of pyrazolo[3,4-d]pyrimidines, pyrrolo[2,3-d]pyrimidines and 6-arylpurines.
Gillespie RJ, Cliffe IA, Dawson CE, Dourish CT, Gaur S, Jordan AM, Knight AR, Lerpiniere J, Misra A, Pratt RM, Roffey J, Stratton GC, Upton R, Weiss SM, Williamson DS.
Bioorg Med Chem Lett (2008) 18 : 2924 -2929
PubMed 18411049 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 67 6.22 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL260146 — — 1 7.89
CHEMBL407049 — — 1 7.77
CHEMBL261203 — — 1 7.77
CHEMBL411034 — — 1 7.58
CHEMBL259049 — — 1 7.58
CHEMBL409915 — — 1 7.55
CHEMBL256344 — — 1 7.33
CHEMBL259164 — — 1 7.22
CHEMBL429144 — — 1 7.16
CHEMBL264432 — — 1 7.12
CHEMBL258181 — — 1 6.91
CHEMBL264431 — — 1 6.90
CHEMBL402409 — — 1 6.89
CHEMBL259832 — — 1 6.77
CHEMBL260337 — — 1 6.76
CHEMBL258006 — — 1 6.71
CHEMBL257757 — — 1 6.69
CHEMBL409682 — — 1 6.64
CHEMBL402172 — — 1 6.60
CHEMBL403252 — — 1 6.58
CHEMBL401973 — — 1 6.55
CHEMBL403470 — — 1 6.50
CHEMBL259210 — — 1 6.33
CHEMBL259418 — — 1 6.33
CHEMBL406298 — — 1 6.32
CHEMBL256360 — — 1 6.30
CHEMBL402389 — — 1 6.30
CHEMBL257982 — — 1 6.29
CHEMBL410033 — — 1 6.27
CHEMBL411473 — — 1 6.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL260146 — Ki = 13.0 nM 7.89
CHEMBL407049 — Ki = 17.0 nM 7.77
CHEMBL261203 — Ki = 17.0 nM 7.77
CHEMBL411034 — Ki = 26.0 nM 7.58
CHEMBL259049 — Ki = 26.0 nM 7.58
CHEMBL409915 — Ki = 28.0 nM 7.55
CHEMBL256344 — Ki = 47.0 nM 7.33
CHEMBL259164 — Ki = 60.0 nM 7.22
CHEMBL429144 — Ki = 70.0 nM 7.16
CHEMBL264432 — Ki = 76.0 nM 7.12
CHEMBL258181 — Ki = 123.0 nM 6.91
CHEMBL264431 — Ki = 127.0 nM 6.90
CHEMBL402409 — Ki = 130.0 nM 6.89
CHEMBL259832 — Ki = 170.0 nM 6.77
CHEMBL260337 — Ki = 175.0 nM 6.76
CHEMBL258006 — Ki = 193.0 nM 6.71
CHEMBL257757 — Ki = 206.0 nM 6.69
CHEMBL409682 — Ki = 231.0 nM 6.64
CHEMBL402172 — Ki = 252.0 nM 6.60
CHEMBL403252 — Ki = 264.0 nM 6.58
CHEMBL401973 — Ki = 284.0 nM 6.55
CHEMBL403470 — Ki = 320.0 nM 6.50
CHEMBL259210 — Ki = 462.0 nM 6.33
CHEMBL259418 — Ki = 468.0 nM 6.33
CHEMBL406298 — Ki = 479.0 nM 6.32
CHEMBL256360 — Ki = 497.0 nM 6.30
CHEMBL402389 — Ki = 504.0 nM 6.30
CHEMBL257982 — Ki = 519.0 nM 6.29
CHEMBL410033 — Ki = 534.0 nM 6.27
CHEMBL411473 — Ki = 547.0 nM 6.26
CHEMBL371615 — Ki = 612.0 nM 6.21
CHEMBL260989 — Ki = 624.0 nM 6.21
CHEMBL260557 — Ki = 647.0 nM 6.19
CHEMBL437804 — Ki = 709.0 nM 6.15
CHEMBL410678 — Ki = 709.0 nM 6.15
CHEMBL257756 — Ki = 721.0 nM 6.14
CHEMBL409152 — Ki = 748.0 nM 6.13
CHEMBL405789 — Ki = 763.0 nM 6.12
CHEMBL256361 — Ki = 779.0 nM 6.11
CHEMBL258960 — Ki = 835.0 nM 6.08
CHEMBL261349 — Ki = 984.0 nM 6.01
CHEMBL261534 — Ki = 1083.0 nM 5.96
CHEMBL402103 — Ki = 1126.0 nM 5.95
CHEMBL260209 — Ki = 1444.0 nM 5.84
CHEMBL267200 — Ki = 1642.0 nM 5.79
CHEMBL256359 — Ki = 1605.0 nM 5.79
CHEMBL256153 — Ki = 1610.0 nM 5.79
CHEMBL371436 — Ki = 1680.0 nM 5.78
CHEMBL410679 — Ki = 1856.0 nM 5.73
CHEMBL259416 — Ki = 1953.0 nM 5.71