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Assay Detail

CHEMBL636729

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Binding
Concentration required for 50% inhibition of [3H]-CHA binding on rat brain adenosine A1 receptor
ChEMBL ↗
47
Total Activities
47
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 (CHEMBL318) ↗
Type SINGLE PROTEIN
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 5.79 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL68738 N6-CYCLOPENTYLADENOSINE — 1 9.00
CHEMBL45891 — — 1 8.30
CHEMBL139000 (R)-PIA — 1 8.30
CHEMBL464859 NECA — 1 7.80
CHEMBL285819 — — 1 7.43
CHEMBL2021340 — — 1 6.73
CHEMBL2374406 — — 1 6.37
CHEMBL2374400 — — 1 6.17
CHEMBL2374391 — — 1 6.16
CHEMBL2374390 — — 1 6.14
CHEMBL98637 — — 1 6.04
CHEMBL2112337 — — 1 6.01
CHEMBL2374395 — — 1 5.90
CHEMBL1256672 — — 1 5.86
CHEMBL2374416 — — 1 5.86
CHEMBL2374412 — — 1 5.78
CHEMBL2374394 — — 1 5.73
CHEMBL2021341 — — 1 5.64
CHEMBL2374408 — — 1 5.64
CHEMBL2374392 — — 1 5.63
CHEMBL87357 — — 1 5.59
CHEMBL314313 — — 1 5.57
CHEMBL2374413 — — 1 5.53
CHEMBL2374411 — — 1 5.44
CHEMBL2374401 — — 1 5.42
CHEMBL2374403 — — 1 5.41
CHEMBL2374393 — — 1 5.41
CHEMBL2374407 — — 1 5.40
CHEMBL2374410 — — 1 5.29
CHEMBL2374396 — — 1 5.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL68738 N6-CYCLOPENTYLADENOSINE IC50 = 1.0 nM 9.00
CHEMBL45891 — IC50 = 5.0 nM 8.30
CHEMBL139000 (R)-PIA IC50 = 5.0 nM 8.30
CHEMBL464859 NECA IC50 = 16.0 nM 7.80
CHEMBL285819 — IC50 = 37.0 nM 7.43
CHEMBL2021340 — IC50 = 186.0 nM 6.73
CHEMBL2374406 — IC50 = 427.0 nM 6.37
CHEMBL2374400 — IC50 = 676.0 nM 6.17
CHEMBL2374391 — IC50 = 692.0 nM 6.16
CHEMBL2374390 — IC50 = 724.0 nM 6.14
CHEMBL98637 — IC50 = 912.0 nM 6.04
CHEMBL2112337 — IC50 = 977.0 nM 6.01
CHEMBL2374395 — IC50 = 1259.0 nM 5.90
CHEMBL1256672 — IC50 = 1380.0 nM 5.86
CHEMBL2374416 — IC50 = 1380.0 nM 5.86
CHEMBL2374412 — IC50 = 1660.0 nM 5.78
CHEMBL2374394 — IC50 = 1862.0 nM 5.73
CHEMBL2021341 — IC50 = 2291.0 nM 5.64
CHEMBL2374408 — IC50 = 2290.0 nM 5.64
CHEMBL2374392 — IC50 = 2344.0 nM 5.63
CHEMBL87357 — IC50 = 2570.0 nM 5.59
CHEMBL314313 — IC50 = 2692.0 nM 5.57
CHEMBL2374413 — IC50 = 2951.0 nM 5.53
CHEMBL2374411 — IC50 = 3631.0 nM 5.44
CHEMBL2374401 — IC50 = 3802.0 nM 5.42
CHEMBL2374403 — IC50 = 3890.0 nM 5.41
CHEMBL2374393 — IC50 = 3890.0 nM 5.41
CHEMBL2374407 — IC50 = 3981.0 nM 5.40
CHEMBL2374410 — IC50 = 5129.0 nM 5.29
CHEMBL2374396 — IC50 = 5248.0 nM 5.28
CHEMBL2374414 — IC50 = 5623.0 nM 5.25
CHEMBL2374405 — IC50 = 5888.0 nM 5.23
CHEMBL2374415 — IC50 = 6918.0 nM 5.16
CHEMBL2374409 — IC50 = 7244.0 nM 5.14
CHEMBL2374398 — IC50 = 7586.0 nM 5.12
CHEMBL2374404 — IC50 = 7586.0 nM 5.12
CHEMBL2374417 — IC50 = 7762.0 nM 5.11
CHEMBL2374397 — IC50 = 8318.0 nM 5.08
CHEMBL2374399 — IC50 = 9772.0 nM 5.01
CHEMBL313069 — IC50 = 10471.0 nM 4.98
CHEMBL87459 — IC50 = 11748.0 nM 4.93
CHEMBL2112107 — IC50 = 12022.0 nM 4.92
CHEMBL88070 — IC50 = 12589.0 nM 4.90
CHEMBL2374418 — IC50 = 13182.0 nM 4.88
CHEMBL86533 — IC50 = 14791.0 nM 4.83
CHEMBL2374419 — IC50 > 10000.0 nM -
CHEMBL2374402 — IC50 > 10000.0 nM -