Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4422945

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

Binding
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL ↗
65
Total Activities
64
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 Autocuration

Target

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

Publication

Novel non-xanthine antagonist of the A<sub>2B</sub> adenosine receptor: From HTS hit to lead structure.
Härter M, Kalthof B, Delbeck M, Lustig K, Gerisch M, Schulz S, Kast R, Meibom D, Lindner N.
Eur J Med Chem (2019) 163 : 763 -778
PubMed 30576906 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 65 6.54 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4569909 — — 1 8.62
CHEMBL4576817 — — 1 8.06
CHEMBL4521489 — — 1 7.92
CHEMBL4458223 — — 1 7.85
CHEMBL4448231 — — 1 7.52
CHEMBL4458042 — — 1 7.41
CHEMBL4449139 — — 1 7.38
CHEMBL4462879 — — 1 7.30
CHEMBL4589448 — — 1 7.26
CHEMBL4474572 — — 1 7.25
CHEMBL4522981 — — 1 7.23
CHEMBL4564912 — — 1 7.14
CHEMBL4516075 — — 1 7.01
CHEMBL4540250 — — 1 7.01
CHEMBL4458469 — — 1 6.89
CHEMBL4540909 — — 1 6.89
CHEMBL4442438 — — 1 6.87
CHEMBL4441343 — — 1 6.84
CHEMBL4457476 — — 1 6.82
CHEMBL4538262 — — 1 6.82
CHEMBL4451942 — — 2 6.75
CHEMBL4553423 — — 1 6.72
CHEMBL4450633 — — 1 6.70
CHEMBL4522738 — — 1 6.70
CHEMBL4452532 — — 1 6.70
CHEMBL4459477 — — 1 6.70
CHEMBL4540558 — — 1 6.68
CHEMBL4440686 — — 1 6.66
CHEMBL4452799 — — 1 6.60
CHEMBL4560841 — — 1 6.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4569909 — IC50 = 2.4 nM 8.62
CHEMBL4576817 — IC50 = 8.8 nM 8.06
CHEMBL4521489 — IC50 = 12.0 nM 7.92
CHEMBL4458223 — IC50 = 14.0 nM 7.85
CHEMBL4448231 — IC50 = 30.0 nM 7.52
CHEMBL4458042 — IC50 = 39.0 nM 7.41
CHEMBL4449139 — IC50 = 42.0 nM 7.38
CHEMBL4462879 — IC50 = 50.0 nM 7.30
CHEMBL4589448 — IC50 = 55.0 nM 7.26
CHEMBL4474572 — IC50 = 56.0 nM 7.25
CHEMBL4522981 — IC50 = 59.0 nM 7.23
CHEMBL4564912 — IC50 = 73.0 nM 7.14
CHEMBL4516075 — IC50 = 97.0 nM 7.01
CHEMBL4540250 — IC50 = 97.0 nM 7.01
CHEMBL4540909 — IC50 = 130.0 nM 6.89
CHEMBL4458469 — IC50 = 130.0 nM 6.89
CHEMBL4442438 — IC50 = 135.0 nM 6.87
CHEMBL4441343 — IC50 = 145.0 nM 6.84
CHEMBL4538262 — IC50 = 150.0 nM 6.82
CHEMBL4457476 — IC50 = 150.0 nM 6.82
CHEMBL4451942 — IC50 = 180.0 nM 6.75
CHEMBL4553423 — IC50 = 190.0 nM 6.72
CHEMBL4452532 — IC50 = 200.0 nM 6.70
CHEMBL4522738 — IC50 = 200.0 nM 6.70
CHEMBL4450633 — IC50 = 200.0 nM 6.70
CHEMBL4459477 — IC50 = 200.0 nM 6.70
CHEMBL4540558 — IC50 = 210.0 nM 6.68
CHEMBL4440686 — IC50 = 220.0 nM 6.66
CHEMBL4452799 — IC50 = 250.0 nM 6.60
CHEMBL4560841 — IC50 = 260.0 nM 6.58
CHEMBL4537687 — IC50 = 280.0 nM 6.55
CHEMBL4528081 — IC50 = 300.0 nM 6.52
CHEMBL4536104 — IC50 = 390.0 nM 6.41
CHEMBL4453228 — IC50 = 390.0 nM 6.41
CHEMBL4446433 — IC50 = 430.0 nM 6.37
CHEMBL4569387 — IC50 = 440.0 nM 6.36
CHEMBL4475483 — IC50 = 440.0 nM 6.36
CHEMBL4543255 — IC50 = 480.0 nM 6.32
CHEMBL4475461 — IC50 = 490.0 nM 6.31
CHEMBL4451942 — IC50 = 520.0 nM 6.28
CHEMBL4541543 — IC50 = 540.0 nM 6.27
CHEMBL4585015 — IC50 = 640.0 nM 6.19
CHEMBL4544040 — IC50 = 760.0 nM 6.12
CHEMBL4518356 — IC50 = 790.0 nM 6.10
CHEMBL4576194 — IC50 = 1100.0 nM 5.96
CHEMBL4589654 — IC50 = 1200.0 nM 5.92
CHEMBL4457584 — IC50 = 1300.0 nM 5.89
CHEMBL4582620 — IC50 = 1500.0 nM 5.82
CHEMBL4450782 — IC50 = 1600.0 nM 5.80
CHEMBL4469697 — IC50 = 1700.0 nM 5.77