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Assay Detail

CHEMBL643181

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Binding
Concentration required for 50% inhibition of [3H]NECA binding on rat brain adenosine A2 receptor
ChEMBL ↗
47
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adenosine A2 receptor (CHEMBL2094117) ↗
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Highly selective adenosine A2 receptor agonists in a series of N-alkylated 2-aminoadenosines.
Francis JE, Webb RL, Ghai GR, Hutchison AJ, Moskal MA, deJesus R, Yokoyama R, Rovinski SL, Contardo N, Dotson R.
J Med Chem (1991) 34 : 2570 -2579
PubMed 1875349 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 47 6.83 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL314313 — — 1 7.89
CHEMBL464859 NECA — 1 7.82
CHEMBL2374391 — — 1 7.77
CHEMBL87459 — — 1 7.66
CHEMBL98637 — — 1 7.64
CHEMBL2021340 — — 1 7.62
CHEMBL2374399 — — 1 7.57
CHEMBL2374394 — — 1 7.52
CHEMBL2374400 — — 1 7.46
CHEMBL2374404 — — 1 7.38
CHEMBL2374393 — — 1 7.38
CHEMBL2374411 — — 1 7.36
CHEMBL2374409 — — 1 7.31
CHEMBL2374390 — — 1 7.29
CHEMBL2374408 — — 1 7.21
CHEMBL2374392 — — 1 7.17
CHEMBL2112337 — — 1 7.17
CHEMBL88070 — — 1 7.13
CHEMBL2374412 — — 1 7.11
CHEMBL2374398 — — 1 7.06
CHEMBL2374416 — — 1 7.05
CHEMBL2374396 — — 1 7.03
CHEMBL2374415 — — 1 6.95
CHEMBL2374406 — — 1 6.92
CHEMBL2374418 — — 1 6.88
CHEMBL2374397 — — 1 6.88
CHEMBL2112107 — — 1 6.86
CHEMBL2374414 — — 1 6.84
CHEMBL1256672 — — 1 6.84
CHEMBL285819 — — 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL314313 — IC50 = 13.0 nM 7.89
CHEMBL464859 NECA IC50 = 15.0 nM 7.82
CHEMBL2374391 — IC50 = 17.0 nM 7.77
CHEMBL87459 — IC50 = 22.0 nM 7.66
CHEMBL98637 — IC50 = 23.0 nM 7.64
CHEMBL2021340 — IC50 = 24.0 nM 7.62
CHEMBL2374399 — IC50 = 27.0 nM 7.57
CHEMBL2374394 — IC50 = 30.0 nM 7.52
CHEMBL2374400 — IC50 = 35.0 nM 7.46
CHEMBL2374404 — IC50 = 42.0 nM 7.38
CHEMBL2374393 — IC50 = 42.0 nM 7.38
CHEMBL2374411 — IC50 = 44.0 nM 7.36
CHEMBL2374409 — IC50 = 49.0 nM 7.31
CHEMBL2374390 — IC50 = 51.0 nM 7.29
CHEMBL2374408 — IC50 = 62.0 nM 7.21
CHEMBL2374392 — IC50 = 68.0 nM 7.17
CHEMBL2112337 — IC50 = 68.0 nM 7.17
CHEMBL88070 — IC50 = 74.0 nM 7.13
CHEMBL2374412 — IC50 = 78.0 nM 7.11
CHEMBL2374398 — IC50 = 87.0 nM 7.06
CHEMBL2374416 — IC50 = 89.0 nM 7.05
CHEMBL2374396 — IC50 = 93.0 nM 7.03
CHEMBL2374415 — IC50 = 112.0 nM 6.95
CHEMBL2374406 — IC50 = 120.0 nM 6.92
CHEMBL2374397 — IC50 = 132.0 nM 6.88
CHEMBL2374418 — IC50 = 132.0 nM 6.88
CHEMBL2112107 — IC50 = 138.0 nM 6.86
CHEMBL2374414 — IC50 = 145.0 nM 6.84
CHEMBL1256672 — IC50 = 145.0 nM 6.84
CHEMBL285819 — IC50 = 160.0 nM 6.80
CHEMBL2374403 — IC50 = 174.0 nM 6.76
CHEMBL2374407 — IC50 = 209.0 nM 6.68
CHEMBL87357 — IC50 = 257.0 nM 6.59
CHEMBL2374413 — IC50 = 288.0 nM 6.54
CHEMBL2374410 — IC50 = 309.0 nM 6.51
CHEMBL139000 (R)-PIA IC50 = 530.0 nM 6.28
CHEMBL2374401 — IC50 = 537.0 nM 6.27
CHEMBL2374395 — IC50 = 589.0 nM 6.23
CHEMBL2374419 — IC50 = 603.0 nM 6.22
CHEMBL2374405 — IC50 = 603.0 nM 6.22
CHEMBL2021341 — IC50 = 794.0 nM 6.10
CHEMBL45891 — IC50 = 790.0 nM 6.10
CHEMBL68738 N6-CYCLOPENTYLADENOSINE IC50 = 1160.0 nM 5.94
CHEMBL2374417 — IC50 = 2399.0 nM 5.62
CHEMBL313069 — IC50 = 5888.0 nM 5.23
CHEMBL86533 — IC50 = 6607.0 nM 5.18
CHEMBL2374402 — IC50 = 11220.0 nM 4.95