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Assay Detail

CHEMBL616540

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

Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
33
Total Activities
33
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 1B (CHEMBL1898)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel potent 5-HT(1F) receptor agonists: structure-activity studies of a series of substituted N-[3-(1-methyl-4-piperidinyl)-1H-pyrrolo[3,2-b]pyridin-5-yl]amides.
Filla SA, Mathes BM, Johnson KW, Phebus LA, Cohen ML, Nelson DL, Zgombick JM, Erickson JA, Schenck KW, Wainscott DB, Branchek TA, Schaus JM.
J Med Chem (2003) 46 : 3060 -3071
PubMed 12825944 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 33 6.42 8.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL105369 1 8.49
CHEMBL323264 1 7.85
CHEMBL105556 1 7.60
CHEMBL101686 1 7.50
CHEMBL103503 1 7.10
CHEMBL104374 1 6.96
CHEMBL105025 1 6.82
CHEMBL101690 1 6.62
CHEMBL431041 1 6.57
CHEMBL104692 1 6.57
CHEMBL104484 1 6.51
CHEMBL105958 1 6.48
CHEMBL420475 1 6.42
CHEMBL321080 1 6.41
CHEMBL103424 1 6.41
CHEMBL105118 1 6.41
CHEMBL419547 1 6.23
CHEMBL105327 1 6.21
CHEMBL321967 1 6.19
CHEMBL105261 1 6.14
CHEMBL321562 1 6.12
CHEMBL318105 1 6.10
CHEMBL105743 1 6.09
CHEMBL102250 1 6.03
CHEMBL104753 1 6.00
CHEMBL105722 1 6.00
CHEMBL105091 1 5.96
CHEMBL449406 1 5.92
CHEMBL103479 1 5.92
CHEMBL103550 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL105369 Ki = 3.2 nM 8.49
CHEMBL323264 Ki = 14.0 nM 7.85
CHEMBL105556 Ki = 25.0 nM 7.60
CHEMBL101686 Ki = 32.0 nM 7.50
CHEMBL103503 Ki = 80.0 nM 7.10
CHEMBL104374 Ki = 110.0 nM 6.96
CHEMBL105025 Ki = 150.0 nM 6.82
CHEMBL101690 Ki = 240.0 nM 6.62
CHEMBL431041 Ki = 270.0 nM 6.57
CHEMBL104692 Ki = 270.0 nM 6.57
CHEMBL104484 Ki = 310.0 nM 6.51
CHEMBL105958 Ki = 330.0 nM 6.48
CHEMBL420475 Ki = 380.0 nM 6.42
CHEMBL105118 Ki = 390.0 nM 6.41
CHEMBL103424 Ki = 390.0 nM 6.41
CHEMBL321080 Ki = 390.0 nM 6.41
CHEMBL419547 Ki = 590.0 nM 6.23
CHEMBL105327 Ki = 610.0 nM 6.21
CHEMBL321967 Ki = 640.0 nM 6.19
CHEMBL105261 Ki = 720.0 nM 6.14
CHEMBL321562 Ki = 750.0 nM 6.12
CHEMBL318105 Ki = 800.0 nM 6.10
CHEMBL105743 Ki = 820.0 nM 6.09
CHEMBL102250 Ki = 930.0 nM 6.03
CHEMBL104753 Ki = 1000.0 nM 6.00
CHEMBL105722 Ki = 1000.0 nM 6.00
CHEMBL105091 Ki = 1100.0 nM 5.96
CHEMBL449406 Ki = 1200.0 nM 5.92
CHEMBL103479 Ki = 1200.0 nM 5.92
CHEMBL103550 Ki = 1600.0 nM 5.80
CHEMBL104720 Ki = 1700.0 nM 5.77
CHEMBL104158 Ki = 2900.0 nM 5.54
CHEMBL320198 Ki = 6000.0 nM 5.22