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Assay Detail

CHEMBL2024732

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Binding
Binding affinity to adenosine A2A receptor by surface plasmon resonance
12
Total Activities
12
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Adenosine receptor A2a (CHEMBL251)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 1,2,4-triazine derivatives as adenosine A(2A) antagonists using structure based drug design.
Congreve M, Andrews SP, Doré AS, Hollenstein K, Hurrell E, Langmead CJ, Mason JS, Ng IW, Tehan B, Zhukov A, Weir M, Marshall FH.
J Med Chem (2012) 55 : 1898 -1903
PubMed 22220592 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 11 7.96 9.80
pKd 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2021950 1 9.80
CHEMBL2024114 1 9.60
CHEMBL2024115 1 8.90
CHEMBL2024118 1 8.50
CHEMBL2024119 1 8.50
CHEMBL2024116 1 8.00
CHEMBL2024117 1 8.00
CHEMBL2024120 1 7.60
CHEMBL2024112 1 7.30
CHEMBL2024111 1 6.40
CHEMBL1370747 1 5.00
CHEMBL2024113 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2021950 Kd = 0.1585 nM 9.80
CHEMBL2024114 Kd = 0.2512 nM 9.60
CHEMBL2024115 Kd = 1.259 nM 8.90
CHEMBL2024118 Kd = 3.162 nM 8.50
CHEMBL2024119 Kd = 3.162 nM 8.50
CHEMBL2024116 Kd = 10.0 nM 8.00
CHEMBL2024117 Kd = 10.0 nM 8.00
CHEMBL2024120 Kd = 25.12 nM 7.60
CHEMBL2024112 Kd = 50.12 nM 7.30
CHEMBL2024111 Kd = 398.11 nM 6.40
CHEMBL1370747 Kd = 10000.0 nM 5.00
CHEMBL2024113 pKd - -