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

CHEMBL643499

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

Binding
Displacement of specific [3H]DPCPX binding at human adenosine A1 receptor expressed in CHO cells
ChEMBL ↗
74
Total Activities
72
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Adenosine receptor A1 (CHEMBL226) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and biological evaluation of new 8-heterocyclic xanthine derivatives as highly potent and selective human A2B adenosine receptor antagonists.
Baraldi PG, Tabrizi MA, Preti D, Bovero A, Romagnoli R, Fruttarolo F, Zaid NA, Moorman AR, Varani K, Gessi S, Merighi S, Borea PA.
J Med Chem (2004) 47 : 1434 -1447
PubMed 14998332 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 74 6.39 7.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL33653 — — 1 7.31
CHEMBL32281 — — 1 7.26
CHEMBL32229 — — 1 7.25
CHEMBL32598 — — 1 7.19
CHEMBL289903 — — 1 7.19
CHEMBL33591 — — 1 7.14
CHEMBL33695 — — 1 7.10
CHEMBL286212 — — 1 7.00
CHEMBL33709 — — 1 6.85
CHEMBL287529 — — 1 6.82
CHEMBL34097 — — 1 6.79
CHEMBL2112067 — — 1 6.78
CHEMBL2112066 — — 1 6.74
CHEMBL33602 — — 1 6.70
CHEMBL32289 — — 1 6.70
CHEMBL260331 — — 1 6.70
CHEMBL33455 — — 2 6.60
CHEMBL32802 — — 1 6.52
CHEMBL32552 — — 1 6.35
CHEMBL32697 — — 1 6.33
CHEMBL32225 — — 1 6.28
CHEMBL555577 — — 1 6.26
CHEMBL32591 — — 1 6.25
CHEMBL33491 — — 1 6.16
CHEMBL32478 — — 1 6.13
CHEMBL32388 — — 1 6.09
CHEMBL32150 — — 1 6.07
CHEMBL32481 — — 1 6.05
CHEMBL286420 — — 1 6.02
CHEMBL32118 — — 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL33653 — Ki = 49.0 nM 7.31
CHEMBL32281 — Ki = 55.0 nM 7.26
CHEMBL32229 — Ki = 56.0 nM 7.25
CHEMBL32598 — Ki = 65.0 nM 7.19
CHEMBL289903 — Ki = 65.0 nM 7.19
CHEMBL33591 — Ki = 72.0 nM 7.14
CHEMBL33695 — Ki = 79.0 nM 7.10
CHEMBL286212 — Ki = 100.0 nM 7.00
CHEMBL33709 — Ki = 140.0 nM 6.85
CHEMBL287529 — Ki = 150.0 nM 6.82
CHEMBL34097 — Ki = 163.0 nM 6.79
CHEMBL2112067 — Ki = 168.0 nM 6.78
CHEMBL2112066 — Ki = 181.0 nM 6.74
CHEMBL32289 — Ki = 200.0 nM 6.70
CHEMBL33602 — Ki = 201.0 nM 6.70
CHEMBL260331 — Ki = 200.0 nM 6.70
CHEMBL33455 — Ki = 250.0 nM 6.60
CHEMBL33455 — Ki = 260.0 nM 6.58
CHEMBL32802 — Ki = 300.0 nM 6.52
CHEMBL32552 — Ki = 448.0 nM 6.35
CHEMBL32697 — Ki = 467.0 nM 6.33
CHEMBL32225 — Ki = 520.0 nM 6.28
CHEMBL555577 — Ki = 548.0 nM 6.26
CHEMBL32591 — Ki = 566.0 nM 6.25
CHEMBL33491 — Ki = 700.0 nM 6.16
CHEMBL32478 — Ki = 746.0 nM 6.13
CHEMBL32388 — Ki = 810.0 nM 6.09
CHEMBL32150 — Ki = 850.0 nM 6.07
CHEMBL32481 — Ki = 900.0 nM 6.05
CHEMBL286420 — Ki = 955.0 nM 6.02
CHEMBL32118 — Ki = 1005.0 nM 6.00
CHEMBL32581 — Ki = 1175.0 nM 5.93
CHEMBL32751 — Ki = 1361.0 nM 5.87
CHEMBL286102 — Ki = 1440.0 nM 5.84
CHEMBL432273 — Ki = 1725.0 nM 5.76
CHEMBL32950 — Ki = 1898.0 nM 5.72
CHEMBL290105 — Ki = 1993.0 nM 5.70
CHEMBL32311 — Ki = 2410.0 nM 5.62
CHEMBL32534 — Ki = 2427.0 nM 5.62
CHEMBL32770 — Ki = 3227.0 nM 5.49
CHEMBL32425 — Ki = 4481.0 nM 5.35
CHEMBL32801 — Ki > 1000.0 nM -
CHEMBL284789 — Ki > 1000.0 nM -
CHEMBL285151 — Ki > 1000.0 nM -
CHEMBL32814 — Ki > 1000.0 nM -
CHEMBL285900 — Ki > 1000.0 nM -
CHEMBL32582 — Ki > 1000.0 nM -
CHEMBL32359 — Ki > 1000.0 nM -
CHEMBL2113342 — Ki > 1000.0 nM -
CHEMBL284615 — Ki > 1000.0 nM -