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Assay Detail

CHEMBL616370

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

Binding
Binding affinity towards Serotonin 5-hydroxytryptamine 1A receptor by displacement of [3H]-(+)-8-OH-DPAT.
9
Total Activities
9
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

Synthesis and biological activities of (R)-5,6-dihydro-N,N-dimethyl-4H-imidazo[4,5,1-ij]quinolin-5-amine and its metabolites.
Heier RF, Dolak LA, Duncan JN, Hyslop DK, Lipton MF, Martin IJ, Mauragis MA, Piercey MF, Nichols NF, Schreur PJ, Smith MW, Moon MW.
J Med Chem (1997) 40 : 639 -646
PubMed 9057850 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.52 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL157138 LISURIDE 3.0 1 9.40
CHEMBL531 PERGOLIDE 4.0 1 8.40
CHEMBL493 BROMOCRIPTINE 4.0 1 7.62
CHEMBL434665 1 7.24
CHEMBL419792 SUMANIROLE 3.0 1 7.14
CHEMBL422344 1 7.04
CHEMBL589 ROPINIROLE 4.0 1 5.77
CHEMBL348285 1 -
CHEMBL345458 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL157138 LISURIDE Ki = 0.4 nM 9.40
CHEMBL531 PERGOLIDE Ki = 4.0 nM 8.40
CHEMBL493 BROMOCRIPTINE Ki = 24.0 nM 7.62
CHEMBL434665 Ki = 58.0 nM 7.24
CHEMBL419792 SUMANIROLE Ki = 73.0 nM 7.14
CHEMBL422344 Ki = 92.0 nM 7.04
CHEMBL589 ROPINIROLE Ki = 1706.0 nM 5.77
CHEMBL348285 Ki > 3257.0 nM -
CHEMBL345458 Ki > 3521.0 nM -