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Assay Detail

CHEMBL643183

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

Binding
Inhibition of binding to Adenosine-2 receptor using [3H]NECA in rat striatum
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Striatum
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adenosine A2 receptor (CHEMBL2094117)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Structure-activity profile of a series of novel triazoloquinazoline adenosine antagonists.
Francis JE, Cash WD, Psychoyos S, Ghai G, Wenk P, Friedmann RC, Atkins C, Warren V, Furness P, Hyun JL.
J Med Chem (1988) 31 : 1014 -1020
PubMed 3361572 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.88 8.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL268431 1 8.48
CHEMBL268550 1 8.26
CHEMBL267015 1 7.72
CHEMBL267415 1 7.57
CHEMBL268867 1 7.25
CHEMBL8136 1 7.21
CHEMBL266095 1 6.94
CHEMBL268615 1 6.84
CHEMBL266267 1 6.80
CHEMBL269785 1 6.75
CHEMBL7266 1 6.28
CHEMBL7551 1 5.92
CHEMBL7748 1 5.89
CHEMBL7511 1 5.80
CHEMBL7897 1 5.54
CHEMBL414023 1 -
CHEMBL7759 1 -
CHEMBL1355736 THEOPHYLLINE 4.0 1 -
CHEMBL7582 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL268431 IC50 = 3.3 nM 8.48
CHEMBL268550 IC50 = 5.5 nM 8.26
CHEMBL267015 IC50 = 19.0 nM 7.72
CHEMBL267415 IC50 = 27.0 nM 7.57
CHEMBL268867 IC50 = 56.0 nM 7.25
CHEMBL8136 IC50 = 61.0 nM 7.21
CHEMBL266095 IC50 = 116.0 nM 6.94
CHEMBL268615 IC50 = 145.0 nM 6.84
CHEMBL266267 IC50 = 158.0 nM 6.80
CHEMBL269785 IC50 = 179.0 nM 6.75
CHEMBL7266 IC50 = 531.0 nM 6.28
CHEMBL7551 IC50 = 1205.0 nM 5.92
CHEMBL7748 IC50 = 1290.0 nM 5.89
CHEMBL7511 IC50 = 1580.0 nM 5.80
CHEMBL7897 IC50 = 2914.0 nM 5.54
CHEMBL414023 IC50 > 10000.0 nM -
CHEMBL7759 IC50 > 10000.0 nM -
CHEMBL1355736 THEOPHYLLINE IC50 > 10000.0 nM -
CHEMBL7582 IC50 > 10000.0 nM -