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Assay Detail

CHEMBL955115

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

Binding
Displacement of [3H]CCPA from human adenosine A1 receptor expressed in CHO cells
50
Total Activities
50
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

8-Bromo-9-alkyl adenine derivatives as tools for developing new adenosine A2A and A2B receptors ligands.
Lambertucci C, Antonini I, Buccioni M, Dal Ben D, Kachare DD, Volpini R, Klotz KN, Cristalli G.
Bioorg Med Chem (2009) 17 : 2812 -2822
PubMed 19282184 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 50 5.41 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 8.40
CHEMBL468633 1 6.55
CHEMBL510288 1 6.24
CHEMBL446264 1 6.08
CHEMBL475455 1 6.00
CHEMBL449924 1 6.00
CHEMBL506450 1 5.96
CHEMBL474058 1 5.82
CHEMBL515419 1 5.66
CHEMBL475617 1 5.54
CHEMBL509367 1 5.51
CHEMBL505089 1 5.50
CHEMBL67199 1 5.37
CHEMBL516238 1 5.34
CHEMBL508561 1 5.31
CHEMBL474207 1 5.31
CHEMBL151071 1 5.17
CHEMBL304009 1 5.13
CHEMBL506888 1 5.08
CHEMBL455493 1 5.06
CHEMBL475023 1 5.03
CHEMBL294590 1 5.00
CHEMBL503376 1 4.92
CHEMBL65976 1 4.92
CHEMBL505633 1 4.80
CHEMBL448396 1 4.70
CHEMBL95897 1 4.54
CHEMBL504495 1 4.54
CHEMBL65747 1 4.48
CHEMBL466044 1 4.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki = 4.0 nM 8.40
CHEMBL468633 Ki = 280.0 nM 6.55
CHEMBL510288 Ki = 570.0 nM 6.24
CHEMBL446264 Ki = 830.0 nM 6.08
CHEMBL475455 Ki = 1000.0 nM 6.00
CHEMBL449924 Ki = 1000.0 nM 6.00
CHEMBL506450 Ki = 1100.0 nM 5.96
CHEMBL474058 Ki = 1500.0 nM 5.82
CHEMBL515419 Ki = 2200.0 nM 5.66
CHEMBL475617 Ki = 2900.0 nM 5.54
CHEMBL509367 Ki = 3100.0 nM 5.51
CHEMBL505089 Ki = 3200.0 nM 5.50
CHEMBL67199 Ki = 4300.0 nM 5.37
CHEMBL516238 Ki = 4600.0 nM 5.34
CHEMBL474207 Ki = 4900.0 nM 5.31
CHEMBL508561 Ki = 4900.0 nM 5.31
CHEMBL151071 Ki = 6700.0 nM 5.17
CHEMBL304009 Ki = 7400.0 nM 5.13
CHEMBL506888 Ki = 8400.0 nM 5.08
CHEMBL455493 Ki = 8700.0 nM 5.06
CHEMBL475023 Ki = 9400.0 nM 5.03
CHEMBL294590 Ki = 10000.0 nM 5.00
CHEMBL503376 Ki = 12000.0 nM 4.92
CHEMBL65976 Ki = 12000.0 nM 4.92
CHEMBL505633 Ki = 16000.0 nM 4.80
CHEMBL448396 Ki = 20000.0 nM 4.70
CHEMBL504495 Ki = 29000.0 nM 4.54
CHEMBL95897 Ki = 29000.0 nM 4.54
CHEMBL65747 Ki = 33000.0 nM 4.48
CHEMBL466044 Ki = 34000.0 nM 4.47
CHEMBL469409 Ki > 100000.0 nM -
CHEMBL449628 Ki > 100000.0 nM -
CHEMBL472147 Ki > 100000.0 nM -
CHEMBL503566 Ki > 100000.0 nM -
CHEMBL475030 Ki > 100000.0 nM -
CHEMBL63783 Ki > 100000.0 nM -
CHEMBL62835 Ki > 100000.0 nM -
CHEMBL474396 Ki > 100000.0 nM -
CHEMBL466850 Ki > 100000.0 nM -
CHEMBL510907 Ki > 100000.0 nM -
CHEMBL445974 Ki > 100000.0 nM -
CHEMBL447623 Ki > 100000.0 nM -
CHEMBL451363 Ki > 100000.0 nM -
CHEMBL475456 Ki > 100000.0 nM -
CHEMBL449346 Ki > 100000.0 nM -
CHEMBL494759 (S)-DHPA Ki > 100000.0 nM -
CHEMBL474623 Ki > 100000.0 nM -
CHEMBL266094 9-BENZYL-9H-ADENINE Ki > 100000.0 nM -
CHEMBL445696 Ki > 100000.0 nM -
CHEMBL449108 Ki > 100000.0 nM -