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Assay Detail

CHEMBL864517

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding affinity to 5HT1A
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 1A (CHEMBL214)
Type SINGLE PROTEIN
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 6.44 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL370863 1 7.72
CHEMBL443567 1 7.19
CHEMBL370125 1 6.95
CHEMBL382057 1 6.91
CHEMBL383564 1 6.80
CHEMBL370594 1 6.53
CHEMBL197968 1 6.48
CHEMBL199875 1 6.40
CHEMBL197656 1 5.99
CHEMBL370136 1 5.97
CHEMBL200802 1 5.84
CHEMBL199876 1 5.82
CHEMBL203362 1 5.81
CHEMBL370364 1 5.74
CHEMBL372222 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL370863 Ki = 19.1 nM 7.72
CHEMBL443567 Ki = 64.9 nM 7.19
CHEMBL370125 Ki = 113.4 nM 6.95
CHEMBL382057 Ki = 122.3 nM 6.91
CHEMBL383564 Ki = 157.3 nM 6.80
CHEMBL370594 Ki = 295.1 nM 6.53
CHEMBL197968 Ki = 333.34 nM 6.48
CHEMBL199875 Ki = 401.3 nM 6.40
CHEMBL197656 Ki = 1030.0 nM 5.99
CHEMBL370136 Ki = 1070.0 nM 5.97
CHEMBL200802 Ki = 1450.0 nM 5.84
CHEMBL199876 Ki = 1513.0 nM 5.82
CHEMBL203362 Ki = 1540.0 nM 5.81
CHEMBL370364 Ki = 1815.0 nM 5.74
CHEMBL372222 Ki > 10000.0 nM -