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Assay Detail

CHEMBL4346832

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

Binding
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

A<sub>2B</sub> Adenosine Receptor Antagonists with Picomolar Potency.
Jiang J, Seel CJ, Temirak A, Namasivayam V, Arridu A, Schabikowski J, Baqi Y, Hinz S, Hockemeyer J, Müller CE.
J Med Chem (2019) 62 : 4032 -4055
PubMed 30835463 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 41 8.92 10.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4552275 1 10.08
CHEMBL4450864 1 9.86
CHEMBL4464522 1 9.83
CHEMBL4540206 1 9.81
CHEMBL4454481 1 9.80
CHEMBL4463929 1 9.67
CHEMBL4466625 1 9.63
CHEMBL4567785 1 9.61
CHEMBL4460114 1 9.47
CHEMBL4530074 1 9.45
CHEMBL4440526 1 9.40
CHEMBL4441276 1 9.39
CHEMBL4454417 1 9.38
CHEMBL4443090 1 9.37
CHEMBL4566170 1 9.32
CHEMBL4456096 1 9.21
CHEMBL4466765 1 9.20
CHEMBL4464175 1 9.20
CHEMBL4471205 1 9.19
CHEMBL4572369 1 9.19
CHEMBL4464738 1 9.15
CHEMBL4453324 1 9.05
CHEMBL4467573 1 8.99
CHEMBL4556744 1 8.91
CHEMBL4437222 1 8.89
CHEMBL4473749 1 8.77
CHEMBL4461478 1 8.72
CHEMBL4537196 1 8.72
CHEMBL4466211 1 8.49
CHEMBL4538468 1 8.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4552275 Ki = 0.0835 nM 10.08
CHEMBL4450864 Ki = 0.137 nM 9.86
CHEMBL4464522 Ki = 0.148 nM 9.83
CHEMBL4540206 Ki = 0.153 nM 9.81
CHEMBL4454481 Ki = 0.159 nM 9.80
CHEMBL4463929 Ki = 0.215 nM 9.67
CHEMBL4466625 Ki = 0.234 nM 9.63
CHEMBL4567785 Ki = 0.244 nM 9.61
CHEMBL4460114 Ki = 0.342 nM 9.47
CHEMBL4530074 Ki = 0.352 nM 9.45
CHEMBL4440526 Ki = 0.397 nM 9.40
CHEMBL4441276 Ki = 0.403 nM 9.39
CHEMBL4454417 Ki = 0.421 nM 9.38
CHEMBL4443090 Ki = 0.432 nM 9.37
CHEMBL4566170 Ki = 0.473 nM 9.32
CHEMBL4456096 Ki = 0.616 nM 9.21
CHEMBL4466765 Ki = 0.632 nM 9.20
CHEMBL4464175 Ki = 0.629 nM 9.20
CHEMBL4471205 Ki = 0.644 nM 9.19
CHEMBL4572369 Ki = 0.643 nM 9.19
CHEMBL4464738 Ki = 0.706 nM 9.15
CHEMBL4453324 Ki = 0.894 nM 9.05
CHEMBL4467573 Ki = 1.02 nM 8.99
CHEMBL4556744 Ki = 1.24 nM 8.91
CHEMBL4437222 Ki = 1.28 nM 8.89
CHEMBL4473749 Ki = 1.69 nM 8.77
CHEMBL4461478 Ki = 1.91 nM 8.72
CHEMBL4537196 Ki = 1.91 nM 8.72
CHEMBL4466211 Ki = 3.22 nM 8.49
CHEMBL4538468 Ki = 3.55 nM 8.45
CHEMBL4547661 Ki = 4.31 nM 8.37
CHEMBL4582353 Ki = 4.3 nM 8.37
CHEMBL4543948 Ki = 5.69 nM 8.24
CHEMBL4445941 Ki = 6.08 nM 8.22
CHEMBL4575279 Ki = 7.02 nM 8.15
CHEMBL4586090 Ki = 7.15 nM 8.15
CHEMBL4583860 Ki = 8.34 nM 8.08
CHEMBL4529435 Ki = 12.2 nM 7.91
CHEMBL4581448 Ki = 18.6 nM 7.73
CHEMBL4455937 Ki = 48.2 nM 7.32
CHEMBL4521715 Ki = 96.7 nM 7.01