Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL616643

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

Binding
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL ↗
40
Total Activities
39
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 1B (CHEMBL1898) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Fluorination of 3-(3-(piperidin-1-yl)propyl)indoles and 3-(3-(piperazin-1-yl)propyl)indoles gives selective human 5-HT1D receptor ligands with improved pharmacokinetic profiles.
van Niel MB, Collins I, Beer MS, Broughton HB, Cheng SK, Goodacre SC, Heald A, Locker KL, MacLeod AM, Morrison D, Moyes CR, O'Connor D, Pike A, Rowley M, Russell MG, Sohal B, Stanton JA, Thomas S, Verrier H, Watt AP, Castro JL.
J Med Chem (1999) 42 : 2087 -2104
PubMed 10377215 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 40 6.70 8.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL65824 — — 1 8.51
CHEMBL65765 — — 1 8.28
CHEMBL65367 — — 1 7.96
CHEMBL2114040 — — 1 7.89
CHEMBL63167 — — 1 7.85
CHEMBL294732 — — 1 7.82
CHEMBL67460 — — 1 7.80
CHEMBL294547 — — 1 7.72
CHEMBL63799 — — 1 7.66
CHEMBL293614 — — 1 7.60
CHEMBL67684 — — 1 7.55
CHEMBL293678 — — 1 7.31
CHEMBL432332 — — 1 7.21
CHEMBL292779 — — 1 7.14
CHEMBL304857 — — 1 6.85
CHEMBL2114038 — — 1 6.77
CHEMBL2115112 — — 1 6.66
CHEMBL2114039 — — 1 6.66
CHEMBL91534 — — 1 6.66
CHEMBL65321 — — 1 6.55
CHEMBL2115111 — — 1 6.52
CHEMBL64004 — — 1 6.51
CHEMBL304197 — — 1 6.44
CHEMBL304833 — — 1 6.42
CHEMBL292262 — — 1 6.28
CHEMBL303514 — — 1 6.27
CHEMBL2114036 — — 1 6.17
CHEMBL304993 — — 1 6.03
CHEMBL63432 — — 2 6.00
CHEMBL65215 — — 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL65824 — IC50 = 3.1 nM 8.51
CHEMBL65765 — IC50 = 5.3 nM 8.28
CHEMBL65367 — IC50 = 11.0 nM 7.96
CHEMBL2114040 — IC50 = 13.0 nM 7.89
CHEMBL63167 — IC50 = 14.0 nM 7.85
CHEMBL294732 — IC50 = 15.0 nM 7.82
CHEMBL67460 — IC50 = 16.0 nM 7.80
CHEMBL294547 — IC50 = 19.0 nM 7.72
CHEMBL63799 — IC50 = 22.0 nM 7.66
CHEMBL293614 — IC50 = 25.0 nM 7.60
CHEMBL67684 — IC50 = 28.0 nM 7.55
CHEMBL293678 — IC50 = 49.0 nM 7.31
CHEMBL432332 — IC50 = 62.0 nM 7.21
CHEMBL292779 — IC50 = 72.0 nM 7.14
CHEMBL304857 — IC50 = 140.0 nM 6.85
CHEMBL2114038 — IC50 = 170.0 nM 6.77
CHEMBL2115112 — IC50 = 220.0 nM 6.66
CHEMBL91534 — IC50 = 220.0 nM 6.66
CHEMBL2114039 — IC50 = 220.0 nM 6.66
CHEMBL65321 — IC50 = 280.0 nM 6.55
CHEMBL2115111 — IC50 = 300.0 nM 6.52
CHEMBL64004 — IC50 = 310.0 nM 6.51
CHEMBL304197 — IC50 = 360.0 nM 6.44
CHEMBL304833 — IC50 = 380.0 nM 6.42
CHEMBL292262 — IC50 = 520.0 nM 6.28
CHEMBL303514 — IC50 = 540.0 nM 6.27
CHEMBL2114036 — IC50 = 680.0 nM 6.17
CHEMBL304993 — IC50 = 930.0 nM 6.03
CHEMBL63258 — IC50 = 1000.0 nM 6.00
CHEMBL65215 — IC50 = 1000.0 nM 6.00
CHEMBL63432 — IC50 = 1000.0 nM 6.00
CHEMBL416688 — IC50 = 1200.0 nM 5.92
CHEMBL63432 — IC50 = 1200.0 nM 5.92
CHEMBL64003 — IC50 = 1300.0 nM 5.89
CHEMBL305301 — IC50 = 1600.0 nM 5.80
CHEMBL433108 — IC50 = 1800.0 nM 5.75
CHEMBL67367 — IC50 = 2100.0 nM 5.68
CHEMBL305062 — IC50 = 3000.0 nM 5.52
CHEMBL68019 — IC50 = 5800.0 nM 5.24
CHEMBL303997 — IC50 = 7200.0 nM 5.14