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Assay Detail

CHEMBL616790

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

Binding
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Frontal cortex
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 1B (CHEMBL3459)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and serotonin receptor affinities of a series of enantiomers of alpha-methyltryptamines: evidence for the binding conformation of tryptamines at serotonin 5-HT1B receptors.
Nichols DE, Lloyd DH, Johnson MP, Hoffman AJ.
J Med Chem (1988) 31 : 1406 -1412
PubMed 3385733 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 6.36 8.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39 SEROTONIN 3.0 1 8.46
CHEMBL8165 5-METHOXYTRYPTAMINE 1 8.19
CHEMBL1416204 1 7.34
CHEMBL1788239 1 6.92
CHEMBL1788281 1 6.42
CHEMBL2093088 1 6.38
CHEMBL1744072 1 6.11
CHEMBL1788285 1 5.86
CHEMBL2093087 1 5.82
CHEMBL1788284 1 5.81
CHEMBL1744073 1 5.67
CHEMBL1788280 1 5.57
CHEMBL1744074 1 5.39
CHEMBL1788282 1 5.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39 SEROTONIN Ki = 3.467 nM 8.46
CHEMBL8165 5-METHOXYTRYPTAMINE Ki = 6.457 nM 8.19
CHEMBL1416204 Ki = 45.71 nM 7.34
CHEMBL1788239 Ki = 120.23 nM 6.92
CHEMBL1788281 Ki = 380.19 nM 6.42
CHEMBL2093088 Ki = 416.87 nM 6.38
CHEMBL1744072 Ki = 776.25 nM 6.11
CHEMBL1788285 Ki = 1380.38 nM 5.86
CHEMBL2093087 Ki = 1513.56 nM 5.82
CHEMBL1788284 Ki = 1548.82 nM 5.81
CHEMBL1744073 Ki = 2137.96 nM 5.67
CHEMBL1788280 Ki = 2691.53 nM 5.57
CHEMBL1744074 Ki = 4073.8 nM 5.39
CHEMBL1788282 Ki = 7244.36 nM 5.14