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Assay Detail

CHEMBL640587

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Binding
Receptor binding affinity for the adenosine A2A receptor was determined using [3H]ZM-241385 as a radioligand in rat
35
Total Activities
35
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 A2a (CHEMBL302)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Structure-affinity relationships of the affinity of 2-pyrazolyl adenosine analogues for the adenosine A2A receptor.
Palle VP, Elzein EO, Gothe SA, Li Z, Gao Z, Meyer S, Blackburn B, Zablocki JA.
Bioorg Med Chem Lett (2002) 12 : 2935 -2939
PubMed 12270178 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 35 6.43 8.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL319387 1 8.66
CHEMBL98603 1 7.85
CHEMBL98659 1 7.30
CHEMBL101218 1 7.22
CHEMBL329712 1 7.22
CHEMBL99169 1 7.22
CHEMBL102116 1 7.18
CHEMBL415118 1 6.85
CHEMBL318928 1 6.72
CHEMBL98597 1 6.72
CHEMBL97937 1 6.68
CHEMBL99983 1 6.66
CHEMBL317052 REGADENOSON ANHYDROUS 4.0 1 6.54
CHEMBL318732 1 6.54
CHEMBL101383 1 6.46
CHEMBL318483 1 6.41
CHEMBL319608 1 6.33
CHEMBL99052 1 5.96
CHEMBL100348 1 5.89
CHEMBL98278 1 5.79
CHEMBL101663 1 5.65
CHEMBL102035 1 5.59
CHEMBL100876 1 5.58
CHEMBL98221 1 5.41
CHEMBL98802 1 5.28
CHEMBL98958 1 5.21
CHEMBL100513 1 4.68
CHEMBL99554 1 -
CHEMBL98849 1 -
CHEMBL319949 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL319387 Ki = 2.2 nM 8.66
CHEMBL98603 Ki = 14.0 nM 7.85
CHEMBL98659 Ki = 50.0 nM 7.30
CHEMBL101218 Ki = 60.0 nM 7.22
CHEMBL329712 Ki = 60.0 nM 7.22
CHEMBL99169 Ki = 60.0 nM 7.22
CHEMBL102116 Ki = 66.0 nM 7.18
CHEMBL415118 Ki = 140.0 nM 6.85
CHEMBL318928 Ki = 190.0 nM 6.72
CHEMBL98597 Ki = 190.0 nM 6.72
CHEMBL97937 Ki = 210.0 nM 6.68
CHEMBL99983 Ki = 220.0 nM 6.66
CHEMBL317052 REGADENOSON ANHYDROUS Ki = 290.0 nM 6.54
CHEMBL318732 Ki = 290.0 nM 6.54
CHEMBL101383 Ki = 350.0 nM 6.46
CHEMBL318483 Ki = 390.0 nM 6.41
CHEMBL319608 Ki = 470.0 nM 6.33
CHEMBL99052 Ki = 1100.0 nM 5.96
CHEMBL100348 Ki = 1280.0 nM 5.89
CHEMBL98278 Ki = 1610.0 nM 5.79
CHEMBL101663 Ki = 2260.0 nM 5.65
CHEMBL102035 Ki = 2590.0 nM 5.59
CHEMBL100876 Ki = 2620.0 nM 5.58
CHEMBL98221 Ki = 3880.0 nM 5.41
CHEMBL98802 Ki = 5290.0 nM 5.28
CHEMBL98958 Ki = 6110.0 nM 5.21
CHEMBL100513 Ki = 21000.0 nM 4.68
CHEMBL99554 Ki > 100000.0 nM -
CHEMBL98849 Ki > 100000.0 nM -
CHEMBL319949 Ki > 100000.0 nM -
CHEMBL328642 Ki > 100000.0 nM -
CHEMBL318264 Ki > 100000.0 nM -
CHEMBL316729 Ki > 100000.0 nM -
CHEMBL98023 Ki > 100000.0 nM -
CHEMBL100992 Ki > 100000.0 nM -