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Assay Detail

CHEMBL4346834

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

Binding
Displacement of [3H]CCPA from recombinant human A1 adenosine receptor expressed in CHO cell membranes measured after 90 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 A1 (CHEMBL226)
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 6.37 6.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4454417 1 6.95
CHEMBL4581448 1 6.72
CHEMBL4437222 1 6.69
CHEMBL4566170 1 6.49
CHEMBL4455937 1 6.48
CHEMBL4582353 1 6.45
CHEMBL4572369 1 6.44
CHEMBL4443090 1 6.38
CHEMBL4567785 1 6.31
CHEMBL4463929 1 6.27
CHEMBL4529435 1 6.25
CHEMBL4440526 1 6.10
CHEMBL4464522 1 6.03
CHEMBL4575279 1 6.00
CHEMBL4473749 1 5.99
CHEMBL4537196 1 -
CHEMBL4466625 1 -
CHEMBL4450864 1 -
CHEMBL4454481 1 -
CHEMBL4456096 1 -
CHEMBL4464738 1 -
CHEMBL4552275 1 -
CHEMBL4586090 1 -
CHEMBL4543948 1 -
CHEMBL4583860 1 -
CHEMBL4445941 1 -
CHEMBL4556744 1 -
CHEMBL4530074 1 -
CHEMBL4461478 1 -
CHEMBL4538468 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4454417 Ki = 113.0 nM 6.95
CHEMBL4581448 Ki = 190.0 nM 6.72
CHEMBL4437222 Ki = 205.0 nM 6.69
CHEMBL4566170 Ki = 326.0 nM 6.49
CHEMBL4455937 Ki = 334.0 nM 6.48
CHEMBL4582353 Ki = 356.0 nM 6.45
CHEMBL4572369 Ki = 364.0 nM 6.44
CHEMBL4443090 Ki = 419.0 nM 6.38
CHEMBL4567785 Ki = 492.0 nM 6.31
CHEMBL4463929 Ki = 535.0 nM 6.27
CHEMBL4529435 Ki = 560.0 nM 6.25
CHEMBL4440526 Ki = 795.0 nM 6.10
CHEMBL4464522 Ki = 928.0 nM 6.03
CHEMBL4575279 Ki = 1010.0 nM 6.00
CHEMBL4473749 Ki = 1036.0 nM 5.99
CHEMBL4547661 Ki > 1000.0 nM -
CHEMBL4540206 Ki > 1000.0 nM -
CHEMBL4521715 Ki > 1000.0 nM -
CHEMBL4453324 Ki > 1000.0 nM -
CHEMBL4464175 Ki > 1000.0 nM -
CHEMBL4467573 Ki > 1000.0 nM -
CHEMBL4471205 Ki > 1000.0 nM -
CHEMBL4466765 Ki > 1000.0 nM -
CHEMBL4466211 Ki > 1000.0 nM -
CHEMBL4460114 Ki > 1000.0 nM -
CHEMBL4441276 Ki > 1000.0 nM -
CHEMBL4537196 Ki > 1000.0 nM -
CHEMBL4466625 Ki > 1000.0 nM -
CHEMBL4450864 Ki > 1000.0 nM -
CHEMBL4454481 Ki > 1000.0 nM -
CHEMBL4456096 Ki > 1000.0 nM -
CHEMBL4464738 Ki > 1000.0 nM -
CHEMBL4552275 Ki > 1000.0 nM -
CHEMBL4586090 Ki > 1000.0 nM -
CHEMBL4543948 Ki > 1000.0 nM -
CHEMBL4583860 Ki >= 1000.0 nM -
CHEMBL4445941 Ki > 1000.0 nM -
CHEMBL4556744 Ki > 1000.0 nM -
CHEMBL4530074 Ki > 1000.0 nM -
CHEMBL4461478 Ki > 1000.0 nM -
CHEMBL4538468 Ki > 1000.0 nM -