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Assay Detail

CHEMBL1046676

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

Binding
Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in HEK293 cells after 120 mins
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

5-hydroxytryptamine receptor 1A (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and characterization of environment-sensitive fluorescent ligands for human 5-HT1A receptors with 1-arylpiperazine structure.
Lacivita E, Leopoldo M, Masotti AC, Inglese C, Berardi F, Perrone R, Ganguly S, Jafurulla M, Chattopadhyay A.
J Med Chem (2009) 52 : 7892 -7896
PubMed 19705871 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 8.06 9.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL574667 1 9.33
CHEMBL591189 1 9.30
CHEMBL8618 NAN-190 1 9.22
CHEMBL578844 1 9.17
CHEMBL31354 WAY-100,635 1 8.66
CHEMBL575762 1 8.17
CHEMBL574894 1 8.11
CHEMBL574239 1 7.82
CHEMBL575763 1 7.54
CHEMBL583707 1 7.36
CHEMBL575991 1 7.27
CHEMBL574903 1 7.14
CHEMBL572935 1 6.94
CHEMBL575768 1 6.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL574667 Ki = 0.47 nM 9.33
CHEMBL591189 Ki = 0.5 nM 9.30
CHEMBL8618 NAN-190 Ki = 0.6 nM 9.22
CHEMBL578844 Ki = 0.67 nM 9.17
CHEMBL31354 WAY-100,635 Ki = 2.2 nM 8.66
CHEMBL575762 Ki = 6.8 nM 8.17
CHEMBL574894 Ki = 7.8 nM 8.11
CHEMBL574239 Ki = 15.0 nM 7.82
CHEMBL575763 Ki = 29.0 nM 7.54
CHEMBL583707 Ki = 44.0 nM 7.36
CHEMBL575991 Ki = 54.0 nM 7.27
CHEMBL574903 Ki = 73.0 nM 7.14
CHEMBL572935 Ki = 116.0 nM 6.94
CHEMBL575768 Ki = 151.0 nM 6.82