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Assay Detail

CHEMBL642011

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

Binding
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
35
Total Activities
35
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 A2b (CHEMBL255)
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 35 7.84 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL416417 1 8.92
CHEMBL37726 1 8.92
CHEMBL38304 1 8.89
CHEMBL36963 1 8.60
CHEMBL34762 1 8.57
CHEMBL416963 1 8.54
CHEMBL284288 1 8.43
CHEMBL40055 1 8.42
CHEMBL35701 1 8.36
CHEMBL274855 1 8.33
CHEMBL38193 1 8.28
CHEMBL37875 1 8.26
CHEMBL37933 1 8.21
CHEMBL37050 1 8.19
CHEMBL286527 1 8.17
CHEMBL288459 1 8.00
CHEMBL37082 1 7.97
CHEMBL8789 1 7.93
CHEMBL286350 1 7.89
CHEMBL37987 1 7.84
CHEMBL34543 1 7.83
CHEMBL2113345 1 7.82
CHEMBL287129 1 7.72
CHEMBL35094 1 7.62
CHEMBL289516 1 7.58
CHEMBL37243 1 7.46
CHEMBL35415 1 7.38
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 7.29
CHEMBL34862 1 7.27
CHEMBL16997 1 7.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL416417 Ki = 1.2 nM 8.92
CHEMBL37726 Ki = 1.2 nM 8.92
CHEMBL38304 Ki = 1.3 nM 8.89
CHEMBL36963 Ki = 2.5 nM 8.60
CHEMBL34762 Ki = 2.7 nM 8.57
CHEMBL416963 Ki = 2.9 nM 8.54
CHEMBL284288 Ki = 3.7 nM 8.43
CHEMBL40055 Ki = 3.8 nM 8.42
CHEMBL35701 Ki = 4.4 nM 8.36
CHEMBL274855 Ki = 4.7 nM 8.33
CHEMBL38193 Ki = 5.3 nM 8.28
CHEMBL37875 Ki = 5.5 nM 8.26
CHEMBL37933 Ki = 6.1 nM 8.21
CHEMBL37050 Ki = 6.5 nM 8.19
CHEMBL286527 Ki = 6.8 nM 8.17
CHEMBL288459 Ki = 10.0 nM 8.00
CHEMBL37082 Ki = 10.8 nM 7.97
CHEMBL8789 Ki = 11.8 nM 7.93
CHEMBL286350 Ki = 13.0 nM 7.89
CHEMBL37987 Ki = 14.5 nM 7.84
CHEMBL34543 Ki = 14.7 nM 7.83
CHEMBL2113345 Ki = 15.1 nM 7.82
CHEMBL287129 Ki = 19.0 nM 7.72
CHEMBL35094 Ki = 24.0 nM 7.62
CHEMBL289516 Ki = 26.0 nM 7.58
CHEMBL37243 Ki = 34.4 nM 7.46
CHEMBL35415 Ki = 42.0 nM 7.38
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki = 51.0 nM 7.29
CHEMBL34862 Ki = 53.4 nM 7.27
CHEMBL16997 Ki = 60.0 nM 7.22
CHEMBL36952 Ki = 70.0 nM 7.16
CHEMBL435575 Ki = 250.0 nM 6.60
CHEMBL37621 Ki = 372.0 nM 6.43
CHEMBL284991 Ki = 520.0 nM 6.28
CHEMBL285191 Ki = 810.0 nM 6.09