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Assay Detail

CHEMBL616919

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

Binding
Binding affinity towards human 5-hydroxytryptamine 1D receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
27
Total Activities
27
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

SAR development of a selective 5-HT1D antagonist/serotonin reuptake inhibitor lead using rapid parallel synthesis.
Timms GH, Boot JR, Broadmore RJ, Carney SL, Cooper J, Findlay JD, Gilmore J, Mitchell S, Moore NA, Pullar I, Sanger GJ, Tomlinson R, Tree BB, Wedley S.
Bioorg Med Chem Lett (2004) 14 : 2469 -2472
PubMed 15109634 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 7.40 8.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL81191 1 8.27
CHEMBL79674 1 8.08
CHEMBL79693 1 7.85
CHEMBL1169435 1 7.82
CHEMBL81703 1 7.70
CHEMBL441259 1 7.62
CHEMBL1159649 1 7.60
CHEMBL83112 1 7.58
CHEMBL83732 1 7.58
CHEMBL2112307 1 7.57
CHEMBL82488 1 7.55
CHEMBL311787 1 7.55
CHEMBL84171 1 7.51
CHEMBL444843 1 7.40
CHEMBL79725 1 7.40
CHEMBL442974 1 7.29
CHEMBL83617 1 7.25
CHEMBL82523 1 7.24
CHEMBL79853 1 7.20
CHEMBL311323 1 7.19
CHEMBL310082 1 7.15
CHEMBL310744 1 7.13
CHEMBL313452 1 6.91
CHEMBL311694 1 6.89
CHEMBL79561 1 6.89
CHEMBL309872 1 6.84
CHEMBL84305 1 6.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL81191 Ki = 5.4 nM 8.27
CHEMBL79674 Ki = 8.4 nM 8.08
CHEMBL79693 Ki = 14.0 nM 7.85
CHEMBL1169435 Ki = 15.0 nM 7.82
CHEMBL81703 Ki = 20.0 nM 7.70
CHEMBL441259 Ki = 24.0 nM 7.62
CHEMBL1159649 Ki = 25.0 nM 7.60
CHEMBL83112 Ki = 26.0 nM 7.58
CHEMBL83732 Ki = 26.0 nM 7.58
CHEMBL2112307 Ki = 27.0 nM 7.57
CHEMBL82488 Ki = 28.0 nM 7.55
CHEMBL311787 Ki = 28.0 nM 7.55
CHEMBL84171 Ki = 31.0 nM 7.51
CHEMBL444843 Ki = 40.0 nM 7.40
CHEMBL79725 Ki = 40.0 nM 7.40
CHEMBL442974 Ki = 51.0 nM 7.29
CHEMBL83617 Ki = 56.0 nM 7.25
CHEMBL82523 Ki = 57.0 nM 7.24
CHEMBL79853 Ki = 63.0 nM 7.20
CHEMBL311323 Ki = 65.0 nM 7.19
CHEMBL310082 Ki = 71.0 nM 7.15
CHEMBL310744 Ki = 74.0 nM 7.13
CHEMBL313452 Ki = 122.0 nM 6.91
CHEMBL311694 Ki = 130.0 nM 6.89
CHEMBL79561 Ki = 130.0 nM 6.89
CHEMBL309872 Ki = 145.0 nM 6.84
CHEMBL84305 Ki = 165.0 nM 6.78