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Assay Detail

CHEMBL1034993

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

Binding
Displacement of [3H]8-OH-DPAT from human cloned 5HT1A receptor expressed in HEK293 cells
25
Total Activities
25
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

Structural modifications of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides: influence on lipophilicity and 5-HT7 receptor activity. Part III.
Leopoldo M, Lacivita E, De Giorgio P, Fracasso C, Guzzetti S, Caccia S, Contino M, Colabufo NA, Berardi F, Perrone R.
J Med Chem (2008) 51 : 5813 -5822
PubMed 18800769 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 7.57 8.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL523381 1 8.97
CHEMBL493305 1 8.69
CHEMBL56 8-OH-DPAT 1 8.68
CHEMBL494316 1 8.49
CHEMBL492282 1 8.43
CHEMBL495321 1 8.09
CHEMBL521687 1 7.99
CHEMBL492691 1 7.92
CHEMBL495120 1 7.89
CHEMBL493709 1 7.72
CHEMBL494119 1 7.66
CHEMBL522194 1 7.54
CHEMBL492690 1 7.40
CHEMBL494512 1 7.37
CHEMBL494312 1 7.28
CHEMBL494661 1 7.24
CHEMBL494709 1 7.16
CHEMBL493909 1 7.03
CHEMBL492480 1 7.02
CHEMBL494458 1 6.97
CHEMBL494118 1 6.91
CHEMBL492872 1 6.86
CHEMBL492871 1 6.79
CHEMBL522691 1 6.73
CHEMBL522343 1 6.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL523381 Ki = 1.07 nM 8.97
CHEMBL493305 Ki = 2.04 nM 8.69
CHEMBL56 8-OH-DPAT Ki = 2.1 nM 8.68
CHEMBL494316 Ki = 3.2 nM 8.49
CHEMBL492282 Ki = 3.7 nM 8.43
CHEMBL495321 Ki = 8.2 nM 8.09
CHEMBL521687 Ki = 10.3 nM 7.99
CHEMBL492691 Ki = 12.0 nM 7.92
CHEMBL495120 Ki = 13.0 nM 7.89
CHEMBL493709 Ki = 19.0 nM 7.72
CHEMBL494119 Ki = 22.0 nM 7.66
CHEMBL522194 Ki = 29.0 nM 7.54
CHEMBL492690 Ki = 40.0 nM 7.40
CHEMBL494512 Ki = 43.0 nM 7.37
CHEMBL494312 Ki = 53.0 nM 7.28
CHEMBL494661 Ki = 57.0 nM 7.24
CHEMBL494709 Ki = 70.0 nM 7.16
CHEMBL493909 Ki = 94.0 nM 7.03
CHEMBL492480 Ki = 95.0 nM 7.02
CHEMBL494458 Ki = 106.0 nM 6.97
CHEMBL494118 Ki = 124.0 nM 6.91
CHEMBL492872 Ki = 139.0 nM 6.86
CHEMBL492871 Ki = 161.0 nM 6.79
CHEMBL522691 Ki = 188.0 nM 6.73
CHEMBL522343 Ki = 325.0 nM 6.49