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Assay Detail

CHEMBL616907

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

Binding
Displacement of [3H]5-HT binding to cloned human 5-hydroxytryptamine 1D receptor stably expressed in CHO cells
61
Total Activities
61
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 1D (CHEMBL1983)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

3-[3-(Piperidin-1-yl)propyl]indoles as highly selective h5-HT(1D) receptor agonists.
Russell MG, Matassa VG, Pengilley RR, van Niel MB, Sohal B, Watt AP, Hitzel L, Beer MS, Stanton JA, Broughton HB, Castro JL.
J Med Chem (1999) 42 : 4981 -5001
PubMed 10585208 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 61 8.34 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL331970 1 9.40
CHEMBL148233 1 9.30
CHEMBL147660 1 9.22
CHEMBL146483 1 9.22
CHEMBL434125 1 9.15
CHEMBL313714 1 9.05
CHEMBL333341 1 9.05
CHEMBL143947 1 9.05
CHEMBL356808 1 8.96
CHEMBL146991 1 8.92
CHEMBL343217 1 8.85
CHEMBL343648 1 8.85
CHEMBL147818 1 8.82
CHEMBL146024 1 8.82
CHEMBL146338 1 8.82
CHEMBL357634 1 8.82
CHEMBL143893 1 8.80
CHEMBL145982 1 8.80
CHEMBL358072 1 8.77
CHEMBL147838 1 8.72
CHEMBL304857 1 8.68
CHEMBL357007 1 8.59
CHEMBL146335 1 8.52
CHEMBL116092 1 8.51
CHEMBL146265 1 8.47
CHEMBL147961 1 8.39
CHEMBL147940 1 8.38
CHEMBL147907 1 8.38
CHEMBL423212 1 8.37
CHEMBL146391 1 8.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL331970 IC50 = 0.4 nM 9.40
CHEMBL148233 IC50 = 0.5 nM 9.30
CHEMBL146483 IC50 = 0.6 nM 9.22
CHEMBL147660 IC50 = 0.6 nM 9.22
CHEMBL434125 IC50 = 0.7 nM 9.15
CHEMBL313714 IC50 = 0.9 nM 9.05
CHEMBL333341 IC50 = 0.9 nM 9.05
CHEMBL143947 IC50 = 0.9 nM 9.05
CHEMBL356808 IC50 = 1.1 nM 8.96
CHEMBL146991 IC50 = 1.2 nM 8.92
CHEMBL343217 IC50 = 1.4 nM 8.85
CHEMBL343648 IC50 = 1.4 nM 8.85
CHEMBL146024 IC50 = 1.5 nM 8.82
CHEMBL147818 IC50 = 1.5 nM 8.82
CHEMBL146338 IC50 = 1.5 nM 8.82
CHEMBL357634 IC50 = 1.5 nM 8.82
CHEMBL143893 IC50 = 1.6 nM 8.80
CHEMBL145982 IC50 = 1.6 nM 8.80
CHEMBL358072 IC50 = 1.7 nM 8.77
CHEMBL147838 IC50 = 1.9 nM 8.72
CHEMBL304857 IC50 = 2.1 nM 8.68
CHEMBL357007 IC50 = 2.6 nM 8.59
CHEMBL146335 IC50 = 3.0 nM 8.52
CHEMBL116092 IC50 = 3.1 nM 8.51
CHEMBL146265 IC50 = 3.4 nM 8.47
CHEMBL147961 IC50 = 4.1 nM 8.39
CHEMBL147907 IC50 = 4.2 nM 8.38
CHEMBL147940 IC50 = 4.2 nM 8.38
CHEMBL423212 IC50 = 4.3 nM 8.37
CHEMBL146391 IC50 = 4.4 nM 8.36
CHEMBL357408 IC50 = 4.5 nM 8.35
CHEMBL117046 IC50 = 4.6 nM 8.34
CHEMBL344537 IC50 = 5.0 nM 8.30
CHEMBL147546 IC50 = 5.7 nM 8.24
CHEMBL147148 IC50 = 5.9 nM 8.23
CHEMBL147979 IC50 = 5.9 nM 8.23
CHEMBL145849 IC50 = 6.0 nM 8.22
CHEMBL143952 IC50 = 6.2 nM 8.21
CHEMBL146129 IC50 = 6.3 nM 8.20
CHEMBL2112862 IC50 = 6.6 nM 8.18
CHEMBL356315 IC50 = 7.6 nM 8.12
CHEMBL343667 IC50 = 8.1 nM 8.09
CHEMBL148085 IC50 = 8.1 nM 8.09
CHEMBL148095 IC50 = 8.9 nM 8.05
CHEMBL434315 IC50 = 9.3 nM 8.03
CHEMBL146023 IC50 = 12.0 nM 7.92
CHEMBL143951 IC50 = 12.0 nM 7.92
CHEMBL145997 IC50 = 14.0 nM 7.85
CHEMBL347570 IC50 = 17.0 nM 7.77
CHEMBL147555 IC50 = 18.0 nM 7.75