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Assay Detail

CHEMBL875909

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

Binding
Binding affinity towards human 5-hydroxytryptamine 1D receptor using [3H]5-HT trifluoroacetate as radioligand
25
Total Activities
25
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 (CHEMBL1983)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Benzylimidazolines as h5-HT1B/1D serotonin receptor ligands: a structure-affinity investigation.
Law H, Dukat M, Teitler M, Lee DK, Mazzocco L, Kamboj R, Rampersad V, Prisinzano T, Glennon RA.
J Med Chem (1998) 41 : 2243 -2251
PubMed 9632357 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 6.90 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL762 OXYMETAZOLINE 4.0 1 9.40
CHEMBL312448 XYLOMETAZOLINE 3.0 1 9.15
CHEMBL308042 1 8.96
CHEMBL70409 1 8.17
CHEMBL73281 1 7.89
CHEMBL72178 1 7.14
CHEMBL307408 1 7.13
CHEMBL72107 1 7.07
CHEMBL308727 1 6.98
CHEMBL73670 1 6.47
CHEMBL309162 1 5.99
CHEMBL303441 1 5.96
CHEMBL72158 1 5.87
CHEMBL72167 1 5.72
CHEMBL71033 1 5.66
CHEMBL73190 1 5.62
CHEMBL73943 1 5.60
CHEMBL309976 1 5.36
CHEMBL770 TOLAZOLINE 4.0 1 -
CHEMBL71751 1 -
CHEMBL56898 1 -
CHEMBL450281 1 -
CHEMBL306940 1 -
CHEMBL73429 1 -
CHEMBL306699 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL762 OXYMETAZOLINE Ki = 0.4 nM 9.40
CHEMBL312448 XYLOMETAZOLINE Ki = 0.7 nM 9.15
CHEMBL308042 Ki = 1.1 nM 8.96
CHEMBL70409 Ki = 6.8 nM 8.17
CHEMBL73281 Ki = 13.0 nM 7.89
CHEMBL72178 Ki = 72.0 nM 7.14
CHEMBL307408 Ki = 74.0 nM 7.13
CHEMBL72107 Ki = 86.0 nM 7.07
CHEMBL308727 Ki = 105.0 nM 6.98
CHEMBL73670 Ki = 340.0 nM 6.47
CHEMBL309162 Ki = 1035.0 nM 5.99
CHEMBL303441 Ki = 1095.0 nM 5.96
CHEMBL72158 Ki = 1360.0 nM 5.87
CHEMBL72167 Ki = 1900.0 nM 5.72
CHEMBL71033 Ki = 2210.0 nM 5.66
CHEMBL73190 Ki = 2375.0 nM 5.62
CHEMBL73943 Ki = 2520.0 nM 5.60
CHEMBL309976 Ki = 4390.0 nM 5.36
CHEMBL770 TOLAZOLINE Ki > 10000.0 nM -
CHEMBL71751 Ki > 10000.0 nM -
CHEMBL56898 Ki > 10000.0 nM -
CHEMBL450281 Ki > 10000.0 nM -
CHEMBL306940 Ki > 10000.0 nM -
CHEMBL73429 Ki > 10000.0 nM -
CHEMBL306699 Ki > 5000.0 nM -