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Assay Detail

CHEMBL829693

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

Binding
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

The discovery of a selective, high affinity A(2B) adenosine receptor antagonist for the potential treatment of asthma.
Zablocki J, Kalla R, Perry T, Palle V, Varkhedkar V, Xiao D, Piscopio A, Maa T, Gimbel A, Hao J, Chu N, Leung K, Zeng D.
Bioorg Med Chem Lett (2005) 15 : 609 -612
PubMed 15664822 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 31 6.21 7.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL368442 1 7.38
CHEMBL180693 1 7.30
CHEMBL180236 1 7.04
CHEMBL361826 1 6.90
CHEMBL181925 1 6.68
CHEMBL178172 1 6.67
CHEMBL362268 1 6.66
CHEMBL183915 1 6.60
CHEMBL178662 1 6.59
CHEMBL183183 1 6.49
CHEMBL181873 1 6.36
CHEMBL360280 1 6.31
CHEMBL180559 1 6.28
CHEMBL181005 1 6.25
CHEMBL181346 1 6.19
CHEMBL367351 1 6.16
CHEMBL181067 1 6.03
CHEMBL360366 1 6.00
CHEMBL181400 1 5.95
CHEMBL181468 1 5.84
CHEMBL263494 1 5.78
CHEMBL179932 1 5.74
CHEMBL180588 1 5.68
CHEMBL182259 1 5.56
CHEMBL181062 1 5.44
CHEMBL434334 1 5.34
CHEMBL180832 1 5.29
CHEMBL179935 1 5.23
CHEMBL180811 1 -
CHEMBL362374 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL368442 Ki = 42.0 nM 7.38
CHEMBL180693 Ki = 50.0 nM 7.30
CHEMBL180236 Ki = 91.0 nM 7.04
CHEMBL361826 Ki = 127.0 nM 6.90
CHEMBL181925 Ki = 207.0 nM 6.68
CHEMBL178172 Ki = 215.0 nM 6.67
CHEMBL362268 Ki = 220.0 nM 6.66
CHEMBL183915 Ki = 250.0 nM 6.60
CHEMBL178662 Ki = 255.0 nM 6.59
CHEMBL183183 Ki = 325.0 nM 6.49
CHEMBL181873 Ki = 438.0 nM 6.36
CHEMBL360280 Ki = 485.0 nM 6.31
CHEMBL180559 Ki = 526.0 nM 6.28
CHEMBL181005 Ki = 557.0 nM 6.25
CHEMBL181346 Ki = 645.0 nM 6.19
CHEMBL367351 Ki = 700.0 nM 6.16
CHEMBL181067 Ki = 945.0 nM 6.03
CHEMBL360366 Ki = 1010.0 nM 6.00
CHEMBL181400 Ki = 1120.0 nM 5.95
CHEMBL181468 Ki = 1450.0 nM 5.84
CHEMBL263494 Ki = 1680.0 nM 5.78
CHEMBL179932 Ki = 1830.0 nM 5.74
CHEMBL180588 Ki = 2080.0 nM 5.68
CHEMBL182259 Ki = 2780.0 nM 5.56
CHEMBL181062 Ki = 3660.0 nM 5.44
CHEMBL434334 Ki = 4520.0 nM 5.34
CHEMBL180832 Ki = 5170.0 nM 5.29
CHEMBL179935 Ki = 5830.0 nM 5.23
CHEMBL180811 Ki > 2000.0 nM -
CHEMBL362374 Ki > 2000.0 nM -
CHEMBL181630 Ki > 6666.0 nM -