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Assay Detail

CHEMBL616301

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

Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1A receptor in CHO-K1 cells
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type CHO-K1
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 1A (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Serotonin dimers: application of the bivalent ligand approach to the design of new potent and selective 5-HT(1B/1D) agonists.
Halazy S, Perez M, Fourrier C, Pallard I, Pauwels PJ, Palmier C, John GW, Valentin JP, Bonnafous R, Martinez J.
J Med Chem (1996) 39 : 4920 -4927
PubMed 8960551 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 8.18 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL148022 1 9.00
CHEMBL144030 1 8.80
CHEMBL342323 1 8.78
CHEMBL424128 1 8.74
CHEMBL147901 1 8.66
CHEMBL147677 1 8.66
CHEMBL39 SEROTONIN 3.0 1 8.61
CHEMBL357830 1 8.40
CHEMBL356277 1 8.39
CHEMBL148314 1 8.37
CHEMBL144397 1 8.07
CHEMBL144128 1 8.02
CHEMBL147851 1 8.02
CHEMBL357478 1 8.01
CHEMBL343196 1 7.84
CHEMBL146720 1 7.70
CHEMBL331240 1 6.87
CHEMBL128 SUMATRIPTAN 4.0 1 6.36
CHEMBL147206 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL148022 Ki = 1.0 nM 9.00
CHEMBL144030 Ki = 1.6 nM 8.80
CHEMBL342323 Ki = 1.66 nM 8.78
CHEMBL424128 Ki = 1.8 nM 8.74
CHEMBL147901 Ki = 2.2 nM 8.66
CHEMBL147677 Ki = 2.2 nM 8.66
CHEMBL39 SEROTONIN Ki = 2.48 nM 8.61
CHEMBL357830 Ki = 4.0 nM 8.40
CHEMBL356277 Ki = 4.06 nM 8.39
CHEMBL148314 Ki = 4.3 nM 8.37
CHEMBL144397 Ki = 8.6 nM 8.07
CHEMBL144128 Ki = 9.5 nM 8.02
CHEMBL147851 Ki = 9.5 nM 8.02
CHEMBL357478 Ki = 9.8 nM 8.01
CHEMBL343196 Ki = 14.3 nM 7.84
CHEMBL146720 Ki = 20.0 nM 7.70
CHEMBL331240 Ki = 134.0 nM 6.87
CHEMBL128 SUMATRIPTAN Ki = 440.0 nM 6.36
CHEMBL147206 Ki > 100.0 nM -