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Assay Detail

CHEMBL619899

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

Binding
Binding affinity for human cloned 5-hydroxytryptamine 7 receptor in HEK 293 using [3H]5-CT as a radioligand
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 7 (CHEMBL3155)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

SB-656104-A: a novel 5-HT(7) receptor antagonist with improved in vivo properties.
Forbes IT, Douglas S, Gribble AD, Ife RJ, Lightfoot AP, Garner AE, Riley GJ, Jeffrey P, Stevens AJ, Stean TO, Thomas DR.
Bioorg Med Chem Lett (2002) 12 : 3341 -3344
PubMed 12392747 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 8.39 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL413707 1 9.30
CHEMBL430706 1 9.17
CHEMBL115262 1 9.15
CHEMBL116292 1 9.10
CHEMBL114345 1 9.08
CHEMBL1256844 1 8.90
CHEMBL323778 1 8.74
CHEMBL330353 1 8.62
CHEMBL331803 1 8.20
CHEMBL111922 1 8.19
CHEMBL112876 1 8.19
CHEMBL113192 1 7.64
CHEMBL112765 1 7.59
CHEMBL112150 1 7.24
CHEMBL111956 1 6.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL413707 Ki = 0.5012 nM 9.30
CHEMBL430706 Ki = 0.6761 nM 9.17
CHEMBL115262 Ki = 0.7079 nM 9.15
CHEMBL116292 Ki = 0.7943 nM 9.10
CHEMBL114345 Ki = 0.8318 nM 9.08
CHEMBL1256844 Ki = 1.259 nM 8.90
CHEMBL323778 Ki = 1.82 nM 8.74
CHEMBL330353 Ki = 2.399 nM 8.62
CHEMBL331803 Ki = 6.31 nM 8.20
CHEMBL111922 Ki = 6.457 nM 8.19
CHEMBL112876 Ki = 6.457 nM 8.19
CHEMBL113192 Ki = 22.91 nM 7.64
CHEMBL112765 Ki = 25.7 nM 7.59
CHEMBL112150 Ki = 57.54 nM 7.24
CHEMBL111956 Ki = 165.96 nM 6.78