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Assay Detail

CHEMBL870844

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

Binding
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
60
Total Activities
60
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

Adenosine receptor A2b (CHEMBL255)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel 1,3-disubstituted 8-(1-benzyl-1H-pyrazol-4-yl) xanthines: high affinity and selective A2B adenosine receptor antagonists.
Kalla RV, Elzein E, Perry T, Li X, Palle V, Varkhedkar V, Gimbel A, Maa T, Zeng D, Zablocki J.
J Med Chem (2006) 49 : 3682 -3692
PubMed 16759111 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 60 7.02 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL208824 1 9.00
CHEMBL273807 1 8.70
CHEMBL426504 1 8.30
CHEMBL380176 1 8.05
CHEMBL254725 1 7.96
CHEMBL210808 1 7.89
CHEMBL251869 1 7.85
CHEMBL251870 1 7.85
CHEMBL210938 1 7.75
CHEMBL380284 1 7.75
CHEMBL210271 1 7.72
CHEMBL378652 1 7.70
CHEMBL207434 1 7.70
CHEMBL379474 1 7.66
CHEMBL378598 1 7.66
CHEMBL261722 1 7.57
CHEMBL210649 1 7.55
CHEMBL209174 1 7.54
CHEMBL210747 1 7.48
CHEMBL210150 1 7.47
CHEMBL210212 1 7.46
CHEMBL378570 1 7.44
CHEMBL208110 1 7.43
CHEMBL210683 1 7.43
CHEMBL380219 1 7.43
CHEMBL408186 1 7.42
CHEMBL207524 1 7.40
CHEMBL210609 1 7.36
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 7.25
CHEMBL210213 1 7.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL208824 Ki = 1.0 nM 9.00
CHEMBL273807 Ki = 2.0 nM 8.70
CHEMBL426504 Ki = 5.0 nM 8.30
CHEMBL380176 Ki = 9.0 nM 8.05
CHEMBL254725 Ki = 11.0 nM 7.96
CHEMBL210808 Ki = 13.0 nM 7.89
CHEMBL251869 Ki = 14.0 nM 7.85
CHEMBL251870 Ki = 14.0 nM 7.85
CHEMBL210938 Ki = 18.0 nM 7.75
CHEMBL380284 Ki = 18.0 nM 7.75
CHEMBL210271 Ki = 19.0 nM 7.72
CHEMBL378652 Ki = 20.0 nM 7.70
CHEMBL207434 Ki = 20.0 nM 7.70
CHEMBL378598 Ki = 22.0 nM 7.66
CHEMBL379474 Ki = 22.0 nM 7.66
CHEMBL261722 Ki = 27.0 nM 7.57
CHEMBL210649 Ki = 28.0 nM 7.55
CHEMBL209174 Ki = 29.0 nM 7.54
CHEMBL210747 Ki = 33.0 nM 7.48
CHEMBL210150 Ki = 34.0 nM 7.47
CHEMBL210212 Ki = 35.0 nM 7.46
CHEMBL378570 Ki = 36.0 nM 7.44
CHEMBL208110 Ki = 37.0 nM 7.43
CHEMBL210683 Ki = 37.0 nM 7.43
CHEMBL380219 Ki = 37.0 nM 7.43
CHEMBL408186 Ki = 38.0 nM 7.42
CHEMBL207524 Ki = 40.0 nM 7.40
CHEMBL210609 Ki = 44.0 nM 7.36
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki = 56.0 nM 7.25
CHEMBL210213 Ki = 58.0 nM 7.24
CHEMBL209217 Ki = 74.0 nM 7.13
CHEMBL210319 Ki = 100.0 nM 7.00
CHEMBL210565 Ki = 200.0 nM 6.70
CHEMBL207482 Ki = 240.0 nM 6.62
CHEMBL208920 Ki = 300.0 nM 6.52
CHEMBL209831 Ki = 310.0 nM 6.51
CHEMBL208723 Ki = 350.0 nM 6.46
CHEMBL210614 Ki = 360.0 nM 6.44
CHEMBL210890 Ki = 390.0 nM 6.41
CHEMBL211038 Ki = 410.0 nM 6.39
CHEMBL210482 Ki = 640.0 nM 6.19
CHEMBL378020 Ki = 650.0 nM 6.19
CHEMBL379032 Ki = 700.0 nM 6.16
CHEMBL383201 Ki = 980.0 nM 6.01
CHEMBL378743 Ki = 990.0 nM 6.00
CHEMBL210738 Ki = 1100.0 nM 5.96
CHEMBL441530 Ki = 1250.0 nM 5.90
CHEMBL379838 Ki = 2100.0 nM 5.68
CHEMBL437301 Ki = 2300.0 nM 5.64
CHEMBL210389 Ki = 3700.0 nM 5.43