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Assay Detail

CHEMBL640535

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Binding
Receptor binding affinity for the adenosine A2A receptor were determined using [3H]ZM-241385 as a radioligand in pig
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine receptor A2a (CHEMBL251)
Type SINGLE PROTEIN
Organism Homo sapiens

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 5.91 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL98659 1 6.92
CHEMBL99169 1 6.42
CHEMBL329712 1 6.42
CHEMBL415118 1 6.36
CHEMBL98597 1 6.31
CHEMBL318928 1 6.25
CHEMBL97937 1 6.15
CHEMBL99983 1 6.06
CHEMBL318732 1 6.01
CHEMBL317052 REGADENOSON ANHYDROUS 4.0 1 5.95
CHEMBL318483 1 5.95
CHEMBL101218 1 5.89
CHEMBL101383 1 5.87
CHEMBL98278 1 5.80
CHEMBL100348 1 5.78
CHEMBL319608 1 5.77
CHEMBL102035 1 5.67
CHEMBL98802 1 5.62
CHEMBL99052 1 5.46
CHEMBL101663 1 5.23
CHEMBL100876 1 5.17
CHEMBL98221 1 5.00
CHEMBL98958 1 -
CHEMBL316729 1 -
CHEMBL328642 1 -
CHEMBL100992 1 -
CHEMBL98849 1 -
CHEMBL99554 1 -
CHEMBL319949 1 -
CHEMBL443495 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL98659 Ki = 120.0 nM 6.92
CHEMBL99169 Ki = 380.0 nM 6.42
CHEMBL329712 Ki = 380.0 nM 6.42
CHEMBL415118 Ki = 440.0 nM 6.36
CHEMBL98597 Ki = 490.0 nM 6.31
CHEMBL318928 Ki = 560.0 nM 6.25
CHEMBL97937 Ki = 710.0 nM 6.15
CHEMBL99983 Ki = 880.0 nM 6.06
CHEMBL318732 Ki = 980.0 nM 6.01
CHEMBL317052 REGADENOSON ANHYDROUS Ki = 1120.0 nM 5.95
CHEMBL318483 Ki = 1120.0 nM 5.95
CHEMBL101218 Ki = 1280.0 nM 5.89
CHEMBL101383 Ki = 1350.0 nM 5.87
CHEMBL98278 Ki = 1580.0 nM 5.80
CHEMBL100348 Ki = 1660.0 nM 5.78
CHEMBL319608 Ki = 1710.0 nM 5.77
CHEMBL102035 Ki = 2140.0 nM 5.67
CHEMBL98802 Ki = 2420.0 nM 5.62
CHEMBL99052 Ki = 3430.0 nM 5.46
CHEMBL101663 Ki = 5900.0 nM 5.23
CHEMBL100876 Ki = 6680.0 nM 5.17
CHEMBL98221 Ki = 10000.0 nM 5.00
CHEMBL317053 Ki > 100000.0 nM -
CHEMBL98023 Ki > 100000.0 nM -
CHEMBL98973 Ki > 100000.0 nM -
CHEMBL318264 Ki > 100000.0 nM -
CHEMBL100513 Ki > 100000.0 nM -
CHEMBL443495 Ki > 100000.0 nM -
CHEMBL319949 Ki > 100000.0 nM -
CHEMBL99554 Ki > 100000.0 nM -
CHEMBL98849 Ki > 100000.0 nM -
CHEMBL100992 Ki > 100000.0 nM -
CHEMBL328642 Ki > 100000.0 nM -
CHEMBL316729 Ki > 100000.0 nM -
CHEMBL98958 Ki > 100000.0 nM -