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Assay Detail

CHEMBL839604

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

Binding
Inhibition of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from rat hippocampus
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Hippocampus
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 1A (CHEMBL273)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis of 3-arylpiperazinylalkylpyrrolo[3,2-d]pyrimidine-2,4-dione derivatives as novel, potent, and selective alpha1-adrenoceptor ligands.
Patanè E, Pittalà V, Guerrera F, Salerno L, Romeo G, Siracusa MA, Russo F, Manetti F, Botta M, Mereghetti I, Cagnotto A, Mennini T.
J Med Chem (2005) 48 : 2420 -2431
PubMed 15801833 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 7.03 7.79

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL190032 1 7.79
CHEMBL190586 1 7.77
CHEMBL192119 1 7.65
CHEMBL192941 1 7.62
CHEMBL193999 1 7.46
CHEMBL301707 1 7.30
CHEMBL192659 1 7.08
CHEMBL192603 1 6.89
CHEMBL426817 1 6.71
CHEMBL190226 1 6.42
CHEMBL190034 1 6.28
CHEMBL190384 1 6.25
CHEMBL415774 1 6.19
CHEMBL372073 1 -
CHEMBL189437 1 -
CHEMBL190301 1 -
CHEMBL191425 1 -
CHEMBL57163 1 -
CHEMBL2113056 1 -
CHEMBL365541 1 -
CHEMBL372222 1 -
CHEMBL190525 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL190032 Ki = 16.14 nM 7.79
CHEMBL190586 Ki = 16.9 nM 7.77
CHEMBL192119 Ki = 22.36 nM 7.65
CHEMBL192941 Ki = 24.01 nM 7.62
CHEMBL193999 Ki = 35.01 nM 7.46
CHEMBL301707 Ki = 50.0 nM 7.30
CHEMBL192659 Ki = 82.99 nM 7.08
CHEMBL192603 Ki = 129.8 nM 6.89
CHEMBL426817 Ki = 192.9 nM 6.71
CHEMBL190226 Ki = 376.2 nM 6.42
CHEMBL190034 Ki = 525.5 nM 6.28
CHEMBL190384 Ki = 558.5 nM 6.25
CHEMBL415774 Ki = 650.6 nM 6.19
CHEMBL372073 Ki > 10000.0 nM -
CHEMBL189437 Ki > 10000.0 nM -
CHEMBL190301 Ki > 10000.0 nM -
CHEMBL191425 Ki > 10000.0 nM -
CHEMBL57163 Ki > 10000.0 nM -
CHEMBL2113056 Ki > 10000.0 nM -
CHEMBL365541 Ki > 10000.0 nM -
CHEMBL372222 Ki > 10000.0 nM -
CHEMBL190525 Ki > 10000.0 nM -