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Assay Detail

CHEMBL641962

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

Binding
Inhibition of [3H]PSB-11 binding to human Adenosine A3 receptor
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine receptor A3 (CHEMBL256)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

1,8-disubstituted xanthine derivatives: synthesis of potent A2B-selective adenosine receptor antagonists.
Hayallah AM, Sandoval-Ramírez J, Reith U, Schobert U, Preiss B, Schumacher B, Daly JW, Müller CE.
J Med Chem (2002) 45 : 1500 -1510
PubMed 11906291 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 6.27 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL16997 1 7.52
CHEMBL284288 1 7.09
CHEMBL37726 1 6.99
CHEMBL35701 1 6.76
CHEMBL435575 1 6.74
CHEMBL35415 1 6.42
CHEMBL416417 1 6.38
CHEMBL38304 1 6.32
CHEMBL286527 1 6.32
CHEMBL38193 1 6.17
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 6.10
CHEMBL287129 1 6.02
CHEMBL289516 1 5.95
CHEMBL286350 1 5.93
CHEMBL37082 1 5.92
CHEMBL37987 1 5.92
CHEMBL284991 1 5.68
CHEMBL2113345 1 5.54
CHEMBL35094 1 5.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL16997 Ki = 30.0 nM 7.52
CHEMBL284288 Ki = 80.6 nM 7.09
CHEMBL37726 Ki = 102.0 nM 6.99
CHEMBL35701 Ki = 173.0 nM 6.76
CHEMBL435575 Ki = 183.0 nM 6.74
CHEMBL35415 Ki = 380.0 nM 6.42
CHEMBL416417 Ki = 422.0 nM 6.38
CHEMBL38304 Ki = 475.0 nM 6.32
CHEMBL286527 Ki = 477.0 nM 6.32
CHEMBL38193 Ki = 676.0 nM 6.17
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki = 795.0 nM 6.10
CHEMBL287129 Ki = 950.0 nM 6.02
CHEMBL289516 Ki = 1119.0 nM 5.95
CHEMBL286350 Ki = 1184.0 nM 5.93
CHEMBL37082 Ki = 1192.0 nM 5.92
CHEMBL37987 Ki = 1217.0 nM 5.92
CHEMBL284991 Ki = 2098.0 nM 5.68
CHEMBL2113345 Ki = 2857.0 nM 5.54
CHEMBL35094 Ki = 4622.0 nM 5.33