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Assay Detail

CHEMBL616742

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

Binding
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1D receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Gorilla gorilla
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 1D (CHEMBL1983)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Isochroman-6-carboxamides as highly selective 5-HT1D agonists: potential new treatment for migraine without cardiovascular side effects.
Ennis MD, Ghazal NB, Hoffman RL, Smith MW, Schlachter SK, Lawson CF, Im WB, Pregenzer JF, Svensson KA, Lewis RA, Hall ED, Sutter DM, Harris LT, McCall RB.
J Med Chem (1998) 41 : 2180 -2183
PubMed 9632349 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 7.94 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL71838 1 9.05
CHEMBL128 SUMATRIPTAN 4.0 1 8.70
CHEMBL71635 1 8.42
CHEMBL71724 1 8.17
CHEMBL69385 1 8.07
CHEMBL71907 1 6.62
CHEMBL71798 1 6.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL71838 Ki = 0.9 nM 9.05
CHEMBL128 SUMATRIPTAN Ki = 2.0 nM 8.70
CHEMBL71635 Ki = 3.8 nM 8.42
CHEMBL71724 Ki = 6.7 nM 8.17
CHEMBL69385 Ki = 8.6 nM 8.07
CHEMBL71907 Ki = 238.0 nM 6.62
CHEMBL71798 Ki = 298.0 nM 6.53