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Assay Detail

CHEMBL990613

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

Binding
Displacement of [3H]5HT from human cloned 5HT1D receptor expressed in CHO cells
16
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Novel 5-HT(1A/1B/1D) receptors antagonists with potent 5-HT reuptake inhibitory activity.
Serafinowska HT, Blaney FE, Lovell PJ, Merlo GG, Scott CM, Smith PW, Starr KR, Watson JM.
Bioorg Med Chem Lett (2008) 18 : 5581 -5585
PubMed 18829312 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 7.19 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL490417 1 9.70
CHEMBL183460 1 8.80
CHEMBL485427 1 8.20
CHEMBL484387 1 8.10
CHEMBL485395 1 8.00
CHEMBL483365 1 7.90
CHEMBL484386 1 7.10
CHEMBL484205 1 6.90
CHEMBL519010 1 6.80
CHEMBL484216 2 6.60
CHEMBL519019 1 6.60
CHEMBL485630 1 6.60
CHEMBL484742 1 5.90
CHEMBL484743 1 5.90
CHEMBL519037 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL490417 Ki = 0.1995 nM 9.70
CHEMBL183460 Ki = 1.585 nM 8.80
CHEMBL485427 Ki = 6.31 nM 8.20
CHEMBL484387 Ki = 7.943 nM 8.10
CHEMBL485395 Ki = 10.0 nM 8.00
CHEMBL483365 Ki = 12.59 nM 7.90
CHEMBL484386 Ki = 79.43 nM 7.10
CHEMBL484205 Ki = 125.89 nM 6.90
CHEMBL519010 Ki = 158.49 nM 6.80
CHEMBL484216 Ki = 251.19 nM 6.60
CHEMBL519019 Ki = 251.19 nM 6.60
CHEMBL485630 Ki = 251.19 nM 6.60
CHEMBL484216 Ki = 501.19 nM 6.30
CHEMBL484742 Ki = 1258.93 nM 5.90
CHEMBL484743 Ki = 1258.93 nM 5.90
CHEMBL519037 Ki = 1995.26 nM 5.70