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Assay Detail

CHEMBL828973

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

Binding
Binding affinity against Adenosine A2a receptor from rat brain tissue was determined using [3H]ZM-241385 as radioligand
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Adenosine receptor A2a (CHEMBL302)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Studies on adenosine A2a receptor antagonists: comparison of three core heterocycles.
Vu CB, Pan D, Peng B, Sha L, Kumaravel G, Jin X, Phadke D, Engber T, Huang C, Reilly J, Tam S, Petter RC.
Bioorg Med Chem Lett (2004) 14 : 4831 -4834
PubMed 15341933 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 7.26 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL174628 1 8.40
CHEMBL360840 1 8.22
CHEMBL183531 1 8.00
CHEMBL360166 1 7.96
CHEMBL353323 1 7.92
CHEMBL435099 1 7.75
CHEMBL184411 1 7.72
CHEMBL177459 1 7.60
CHEMBL17127 SCH-58261 1 7.43
CHEMBL426782 1 7.43
CHEMBL359641 1 7.41
CHEMBL186562 1 7.36
CHEMBL184002 1 7.24
CHEMBL177386 1 7.22
CHEMBL362310 1 7.10
CHEMBL182505 1 7.00
CHEMBL184233 1 6.95
CHEMBL185497 1 6.90
CHEMBL363235 1 6.83
CHEMBL187058 1 6.73
CHEMBL184602 1 6.72
CHEMBL182754 1 6.51
CHEMBL186960 1 6.44
CHEMBL186594 1 6.40
CHEMBL362743 1 6.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL174628 Ki = 4.0 nM 8.40
CHEMBL360840 Ki = 6.0 nM 8.22
CHEMBL183531 Ki = 10.0 nM 8.00
CHEMBL360166 Ki = 11.0 nM 7.96
CHEMBL353323 Ki = 12.0 nM 7.92
CHEMBL435099 Ki = 18.0 nM 7.75
CHEMBL184411 Ki = 19.0 nM 7.72
CHEMBL177459 Ki = 25.0 nM 7.60
CHEMBL17127 SCH-58261 Ki = 37.0 nM 7.43
CHEMBL426782 Ki = 37.0 nM 7.43
CHEMBL359641 Ki = 39.0 nM 7.41
CHEMBL186562 Ki = 44.0 nM 7.36
CHEMBL184002 Ki = 57.0 nM 7.24
CHEMBL177386 Ki = 60.0 nM 7.22
CHEMBL362310 Ki = 79.0 nM 7.10
CHEMBL182505 Ki = 100.0 nM 7.00
CHEMBL184233 Ki = 112.0 nM 6.95
CHEMBL185497 Ki = 127.0 nM 6.90
CHEMBL363235 Ki = 148.0 nM 6.83
CHEMBL187058 Ki = 187.0 nM 6.73
CHEMBL184602 Ki = 192.0 nM 6.72
CHEMBL182754 Ki = 312.0 nM 6.51
CHEMBL186960 Ki = 366.0 nM 6.44
CHEMBL186594 Ki = 397.0 nM 6.40
CHEMBL362743 Ki = 659.0 nM 6.18