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Assay Detail

CHEMBL828276

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Binding
Inhibition of [3H]ZM-241385 binding to adenosine A2a receptor of rat brain tissue
ChEMBL ↗
56
Total Activities
56
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

Novel diamino derivatives of [1,2,4]triazolo[1,5-a][1,3,5]triazine as potent and selective adenosine A2a receptor antagonists.
Vu CB, Pan D, Peng B, Kumaravel G, Smits G, Jin X, Phadke D, Engber T, Huang C, Reilly J, Tam S, Grant D, Hetu G, Petter RC.
J Med Chem (2005) 48 : 2009 -2018
PubMed 15771443 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 56 7.62 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL113142 ZM-241385 — 1 9.05
CHEMBL176039 — — 1 8.70
CHEMBL173941 — — 1 8.52
CHEMBL179478 — — 1 8.52
CHEMBL173672 — — 1 8.40
CHEMBL176071 — — 1 8.40
CHEMBL177615 — — 1 8.40
CHEMBL174628 — — 1 8.40
CHEMBL177446 — — 1 8.40
CHEMBL368201 — — 1 8.30
CHEMBL177532 — — 1 8.30
CHEMBL369373 — — 1 8.15
CHEMBL369070 — — 1 8.15
CHEMBL173993 — — 1 8.15
CHEMBL177859 — — 1 8.10
CHEMBL367593 — — 1 8.10
CHEMBL368070 — — 1 7.96
CHEMBL177539 — — 1 7.92
CHEMBL353323 — — 1 7.92
CHEMBL177943 — — 1 7.85
CHEMBL366472 — — 1 7.85
CHEMBL175645 — — 1 7.85
CHEMBL175564 — — 1 7.82
CHEMBL177229 — — 1 7.77
CHEMBL369550 — — 1 7.75
CHEMBL368619 — — 1 7.75
CHEMBL177386 — — 1 7.66
CHEMBL177459 — — 1 7.60
CHEMBL177609 — — 1 7.60
CHEMBL175818 — — 1 7.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL113142 ZM-241385 Ki = 0.9 nM 9.05
CHEMBL176039 — Ki = 2.0 nM 8.70
CHEMBL179478 — Ki = 3.0 nM 8.52
CHEMBL173941 — Ki = 3.0 nM 8.52
CHEMBL173672 — Ki = 4.0 nM 8.40
CHEMBL176071 — Ki = 4.0 nM 8.40
CHEMBL177615 — Ki = 4.0 nM 8.40
CHEMBL174628 — Ki = 4.0 nM 8.40
CHEMBL177446 — Ki = 4.0 nM 8.40
CHEMBL368201 — Ki = 5.0 nM 8.30
CHEMBL177532 — Ki = 5.0 nM 8.30
CHEMBL173993 — Ki = 7.0 nM 8.15
CHEMBL369070 — Ki = 7.0 nM 8.15
CHEMBL369373 — Ki = 7.0 nM 8.15
CHEMBL367593 — Ki = 8.0 nM 8.10
CHEMBL177859 — Ki = 8.0 nM 8.10
CHEMBL368070 — Ki = 11.0 nM 7.96
CHEMBL177539 — Ki = 12.0 nM 7.92
CHEMBL353323 — Ki = 12.0 nM 7.92
CHEMBL177943 — Ki = 14.0 nM 7.85
CHEMBL366472 — Ki = 14.0 nM 7.85
CHEMBL175645 — Ki = 14.0 nM 7.85
CHEMBL175564 — Ki = 15.0 nM 7.82
CHEMBL177229 — Ki = 17.0 nM 7.77
CHEMBL368619 — Ki = 18.0 nM 7.75
CHEMBL369550 — Ki = 18.0 nM 7.75
CHEMBL177386 — Ki = 22.0 nM 7.66
CHEMBL177459 — Ki = 25.0 nM 7.60
CHEMBL177609 — Ki = 25.0 nM 7.60
CHEMBL175818 — Ki = 30.0 nM 7.52
CHEMBL368382 — Ki = 30.0 nM 7.52
CHEMBL368620 — Ki = 36.0 nM 7.44
CHEMBL17127 SCH-58261 Ki = 37.0 nM 7.43
CHEMBL426782 — Ki = 37.0 nM 7.43
CHEMBL175298 — Ki = 39.0 nM 7.41
CHEMBL359641 — Ki = 39.0 nM 7.41
CHEMBL27508 — Ki = 42.0 nM 7.38
CHEMBL175569 — Ki = 52.0 nM 7.28
CHEMBL368827 — Ki = 57.0 nM 7.24
CHEMBL2112968 — Ki = 64.0 nM 7.19
CHEMBL177654 — Ki = 79.0 nM 7.10
CHEMBL177449 — Ki = 130.0 nM 6.89
CHEMBL425685 — Ki = 150.0 nM 6.82
CHEMBL177711 — Ki = 180.0 nM 6.75
CHEMBL175927 — Ki = 180.0 nM 6.75
CHEMBL175713 — Ki = 200.0 nM 6.70
CHEMBL368092 — Ki = 270.0 nM 6.57
CHEMBL361229 — Ki = 516.0 nM 6.29
CHEMBL368983 — Ki = 560.0 nM 6.25
CHEMBL177710 — Ki = 680.0 nM 6.17