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Assay Detail

CHEMBL640605

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Binding
Binding affinity against bovine brain adenosine A1 receptor by using N6-[3H]- cyclohexyladenosine
ChEMBL ↗
76
Total Activities
76
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine receptor A1 (CHEMBL4975) ↗
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Synthesis of xanthines as adenosine antagonists, a practical quantitative structure-activity relationship application.
Hamilton HW, Ortwine DF, Worth DF, Badger EW, Bristol JA, Bruns RF, Haleen SJ, Steffen RP.
J Med Chem (1985) 28 : 1071 -1079
PubMed 2991519 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 76 8.23 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL11002 — — 1 10.30
CHEMBL273671 — — 1 10.30
CHEMBL545362 — — 1 10.15
CHEMBL11036 — — 1 10.10
CHEMBL415971 — — 1 9.82
CHEMBL11173 — — 1 9.62
CHEMBL268964 — — 1 9.46
CHEMBL158507 — — 1 9.15
CHEMBL275263 — — 1 9.12
CHEMBL11104 — — 1 9.12
CHEMBL269218 — — 1 9.10
CHEMBL11410 — — 1 9.10
CHEMBL11127 — — 1 9.10
CHEMBL10995 — — 1 9.10
CHEMBL268026 — — 1 9.10
CHEMBL11027 — — 1 9.04
CHEMBL11342 — — 1 9.00
CHEMBL11271 — — 1 8.89
CHEMBL11635 — — 1 8.82
CHEMBL10913 — — 1 8.80
CHEMBL276830 — — 1 8.76
CHEMBL11332 — — 1 8.74
CHEMBL27047 — — 1 8.70
CHEMBL11163 — — 1 8.70
CHEMBL268701 — — 1 8.70
CHEMBL276603 — — 1 8.70
CHEMBL10895 — — 1 8.60
CHEMBL11037 — — 1 8.60
CHEMBL9069 — — 1 8.60
CHEMBL62350 8-PHENYL THEOPHYLLINE — 1 8.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL11002 — IC50 = 0.05 nM 10.30
CHEMBL273671 — IC50 = 0.05 nM 10.30
CHEMBL545362 — IC50 = 0.07 nM 10.15
CHEMBL11036 — IC50 = 0.08 nM 10.10
CHEMBL415971 — IC50 = 0.15 nM 9.82
CHEMBL11173 — IC50 = 0.24 nM 9.62
CHEMBL268964 — IC50 = 0.35 nM 9.46
CHEMBL158507 — IC50 = 0.7 nM 9.15
CHEMBL275263 — IC50 = 0.75 nM 9.12
CHEMBL11104 — IC50 = 0.75 nM 9.12
CHEMBL11127 — IC50 = 0.8 nM 9.10
CHEMBL268026 — IC50 = 0.8 nM 9.10
CHEMBL10995 — IC50 = 0.8 nM 9.10
CHEMBL11410 — IC50 = 0.8 nM 9.10
CHEMBL269218 — IC50 = 0.8 nM 9.10
CHEMBL11027 — IC50 = 0.91 nM 9.04
CHEMBL11342 — IC50 = 1.0 nM 9.00
CHEMBL11271 — IC50 = 1.3 nM 8.89
CHEMBL11635 — IC50 = 1.5 nM 8.82
CHEMBL10913 — IC50 = 1.6 nM 8.80
CHEMBL276830 — IC50 = 1.75 nM 8.76
CHEMBL11332 — IC50 = 1.8 nM 8.74
CHEMBL276603 — IC50 = 2.0 nM 8.70
CHEMBL268701 — IC50 = 2.0 nM 8.70
CHEMBL27047 — IC50 = 2.0 nM 8.70
CHEMBL11163 — IC50 = 2.0 nM 8.70
CHEMBL10895 — IC50 = 2.5 nM 8.60
CHEMBL11037 — IC50 = 2.5 nM 8.60
CHEMBL9069 — IC50 = 2.5 nM 8.60
CHEMBL62350 8-PHENYL THEOPHYLLINE IC50 = 3.0 nM 8.52
CHEMBL11348 — IC50 = 3.0 nM 8.52
CHEMBL276201 — IC50 = 3.3 nM 8.48
CHEMBL273295 — IC50 = 3.3 nM 8.48
CHEMBL418333 — IC50 = 3.4 nM 8.47
CHEMBL273267 — IC50 = 3.5 nM 8.46
CHEMBL276401 — IC50 = 3.5 nM 8.46
CHEMBL11077 — IC50 = 4.0 nM 8.40
CHEMBL10873 — IC50 = 4.0 nM 8.40
CHEMBL11220 — IC50 = 4.0 nM 8.40
CHEMBL11206 — IC50 = 4.2 nM 8.38
CHEMBL11288 — IC50 = 5.0 nM 8.30
CHEMBL275793 — IC50 = 5.5 nM 8.26
CHEMBL11120 — IC50 = 5.5 nM 8.26
CHEMBL11054 — IC50 = 6.0 nM 8.22
CHEMBL11049 — IC50 = 6.5 nM 8.19
CHEMBL10937 — IC50 = 6.5 nM 8.19
CHEMBL10984 — IC50 = 7.0 nM 8.15
CHEMBL11000 — IC50 = 8.0 nM 8.10
CHEMBL416884 — IC50 = 8.0 nM 8.10
CHEMBL406993 — IC50 = 10.0 nM 8.00