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Assay Detail

CHEMBL864516

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Binding
Binding affinity to adrenergic alpha-1 receptor
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adrenergic receptor alpha-1 (CHEMBL2094251)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

3-Arylpiperazinylethyl-1H-pyrrolo[2,3-d]pyrimidine-2,4(3H,7H)-dione derivatives as novel, high-affinity and selective alpha(1)-adrenoceptor ligands.
Pittalà V, Romeo G, Salerno L, Siracusa MA, Modica M, Materia L, Mereghetti I, Cagnotto A, Mennini T, Marucci G, Angeli P, Russo F.
Bioorg Med Chem Lett (2006) 16 : 150 -153
PubMed 16216506 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 8.38 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL370594 1 8.92
CHEMBL383564 1 8.79
CHEMBL382057 1 8.70
CHEMBL370863 1 8.66
CHEMBL199876 1 8.58
CHEMBL200802 1 8.55
CHEMBL197656 1 8.48
CHEMBL199875 1 8.39
CHEMBL203362 1 8.33
CHEMBL197968 1 8.30
CHEMBL370125 1 8.26
CHEMBL443567 1 8.20
CHEMBL370364 1 7.93
CHEMBL370136 1 7.79
CHEMBL372222 1 7.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL370594 Ki = 1.19 nM 8.92
CHEMBL383564 Ki = 1.63 nM 8.79
CHEMBL382057 Ki = 1.99 nM 8.70
CHEMBL370863 Ki = 2.18 nM 8.66
CHEMBL199876 Ki = 2.64 nM 8.58
CHEMBL200802 Ki = 2.8 nM 8.55
CHEMBL197656 Ki = 3.32 nM 8.48
CHEMBL199875 Ki = 4.08 nM 8.39
CHEMBL203362 Ki = 4.71 nM 8.33
CHEMBL197968 Ki = 4.97 nM 8.30
CHEMBL370125 Ki = 5.47 nM 8.26
CHEMBL443567 Ki = 6.28 nM 8.20
CHEMBL370364 Ki = 11.71 nM 7.93
CHEMBL370136 Ki = 16.4 nM 7.79
CHEMBL372222 Ki = 17.26 nM 7.76