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Assay Detail

CHEMBL3414155

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

Binding
Displacement of [3H]-8-OH-DPAT from human 5HT1A receptor expressed in HEK293 cells after 1 hr
22
Total Activities
22
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 Autocuration

Target

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

Publication

Towards novel 5-HT7versus 5-HT1A receptor ligands among LCAPs with cyclic amino acid amide fragments: design, synthesis, and antidepressant properties. Part II.
Canale V, Kurczab R, Partyka A, Satała G, Witek J, Jastrzębska-Więsek M, Pawłowski M, Bojarski AJ, Wesołowska A, Zajdel P.
Eur J Med Chem (2015) 92 : 202 -211
PubMed 25555143 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 7.63 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3409037 1 9.00
CHEMBL3409041 1 8.05
CHEMBL3409044 1 7.85
CHEMBL3409043 1 7.80
CHEMBL3409031 1 7.80
CHEMBL3409049 1 7.80
CHEMBL3409038 1 7.77
CHEMBL3409040 1 7.75
CHEMBL3409047 1 7.72
CHEMBL3409034 1 7.70
CHEMBL3409036 1 7.58
CHEMBL3409033 1 7.47
CHEMBL3409042 1 7.46
CHEMBL3409039 1 7.46
CHEMBL3409046 1 7.44
CHEMBL3409048 1 7.40
CHEMBL3409045 1 7.33
CHEMBL225284 1 7.28
CHEMBL3409032 1 7.28
CHEMBL3407516 1 7.21
CHEMBL3409035 1 7.18
CHEMBL3235744 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3409037 Ki = 1.0 nM 9.00
CHEMBL3409041 Ki = 9.0 nM 8.05
CHEMBL3409044 Ki = 14.0 nM 7.85
CHEMBL3409043 Ki = 16.0 nM 7.80
CHEMBL3409031 Ki = 16.0 nM 7.80
CHEMBL3409049 Ki = 16.0 nM 7.80
CHEMBL3409038 Ki = 17.0 nM 7.77
CHEMBL3409040 Ki = 18.0 nM 7.75
CHEMBL3409047 Ki = 19.0 nM 7.72
CHEMBL3409034 Ki = 20.0 nM 7.70
CHEMBL3409036 Ki = 26.0 nM 7.58
CHEMBL3409033 Ki = 34.0 nM 7.47
CHEMBL3409042 Ki = 35.0 nM 7.46
CHEMBL3409039 Ki = 35.0 nM 7.46
CHEMBL3409046 Ki = 36.0 nM 7.44
CHEMBL3409048 Ki = 40.0 nM 7.40
CHEMBL3409045 Ki = 47.0 nM 7.33
CHEMBL225284 Ki = 52.7 nM 7.28
CHEMBL3409032 Ki = 53.0 nM 7.28
CHEMBL3407516 Ki = 61.0 nM 7.21
CHEMBL3409035 Ki = 66.0 nM 7.18
CHEMBL3235744 Ki < 1.0 nM -