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Assay Detail

CHEMBL617579

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Binding
Binding affinity was measured against serotonin 5-hydroxytryptamine 1D receptor
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 1D (CHEMBL5450)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

5-[(3-nitropyrid-2-yl)amino]indoles: novel serotonin agonists with selectivity for the 5-HT1D receptor. Variation of the C3 substituent on the indole template leads to increased 5-HT1D receptor selectivity.
Macor JE, Blank DH, Fox CB, Lebel LA, Newman ME, Post RJ, Ryan K, Schmidt AW, Schulz DW, Koe BK.
J Med Chem (1994) 37 : 2509 -2512
PubMed 8057297 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.05 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39 SEROTONIN 3.0 1 8.52
CHEMBL83597 1 8.51
CHEMBL84107 1 8.21
CHEMBL314213 1 8.00
CHEMBL84942 1 7.82
CHEMBL128 SUMATRIPTAN 4.0 1 7.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39 SEROTONIN IC50 = 3.0 nM 8.52
CHEMBL83597 IC50 = 3.1 nM 8.51
CHEMBL84107 IC50 = 6.2 nM 8.21
CHEMBL314213 IC50 = 10.0 nM 8.00
CHEMBL84942 IC50 = 15.0 nM 7.82
CHEMBL128 SUMATRIPTAN IC50 = 61.0 nM 7.21