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Assay Detail

CHEMBL617583

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

Binding
Binding affinity to 5-hydroxytryptamine 1D receptor in the rat forebrain by [3H]- SB-204269 displacement.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Identification of (-)-cis-6-acetyl-4S-(3-chloro-4-fluoro-benzoylamino)- 3,4-dihydro-2,2-dimethyl-2H-benzo[b]pyran-3S-ol as a potential antimigraine agent.
Chan WN, Evans JM, Hadley MS, Herdon HJ, Jerman JC, Parsons AA, Read SJ, Stean TO, Thompson M, Upton N.
Bioorg Med Chem Lett (1999) 9 : 285 -290
PubMed 10021946 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.21 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL95387 1 8.00
CHEMBL98434 1 8.00
CHEMBL38918 1 7.90
CHEMBL318906 1 7.90
CHEMBL318022 1 7.80
CHEMBL318882 1 7.80
CHEMBL98433 1 7.70
CHEMBL317732 1 7.50
CHEMBL316885 1 7.50
CHEMBL99341 1 7.50
CHEMBL98388 1 7.10
CHEMBL98195 1 6.80
CHEMBL99584 1 6.50
CHEMBL95250 1 5.30
CHEMBL433377 1 4.80
CHEMBL98214 1 -
CHEMBL100521 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL95387 Ki = 10.0 nM 8.00
CHEMBL98434 Ki = 10.0 nM 8.00
CHEMBL38918 Ki = 12.59 nM 7.90
CHEMBL318906 Ki = 12.59 nM 7.90
CHEMBL318022 Ki = 15.85 nM 7.80
CHEMBL318882 Ki = 15.85 nM 7.80
CHEMBL98433 Ki = 19.95 nM 7.70
CHEMBL317732 Ki = 31.62 nM 7.50
CHEMBL316885 Ki = 31.62 nM 7.50
CHEMBL99341 Ki = 31.62 nM 7.50
CHEMBL98388 Ki = 79.43 nM 7.10
CHEMBL98195 Ki = 158.49 nM 6.80
CHEMBL99584 Ki = 316.23 nM 6.50
CHEMBL95250 Ki = 5011.87 nM 5.30
CHEMBL433377 Ki = 15848.93 nM 4.80
CHEMBL98214 Ki < 31622.78 nM -
CHEMBL100521 Ki < 6309.57 nM -