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Assay Detail

CHEMBL895655

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

Binding
Binding affinity to human 5HT1A receptor
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3 receptor ligands: potential substance abuse therapeutic agents.
Grundt P, Prevatt KM, Cao J, Taylor M, Floresca CZ, Choi JK, Jenkins BG, Luedtke RR, Newman AH.
J Med Chem (2007) 50 : 4135 -4146
PubMed 17672446 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 7.00 8.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL241973 1 8.17
CHEMBL390253 1 7.82
CHEMBL394541 1 7.66
CHEMBL69451 1 7.63
CHEMBL244562 1 7.53
CHEMBL110365 1 7.47
CHEMBL244990 1 7.46
CHEMBL242644 1 7.44
CHEMBL231156 1 7.23
CHEMBL244774 1 7.22
CHEMBL244989 1 7.14
CHEMBL180010 1 7.07
CHEMBL244773 1 7.04
CHEMBL242434 1 6.93
CHEMBL398175 1 6.51
CHEMBL244775 1 6.18
CHEMBL304605 1 6.03
CHEMBL394863 1 6.01
CHEMBL396024 1 5.74
CHEMBL300780 1 5.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL241973 Ki = 6.71 nM 8.17
CHEMBL390253 Ki = 15.1 nM 7.82
CHEMBL394541 Ki = 21.7 nM 7.66
CHEMBL69451 Ki = 23.4 nM 7.63
CHEMBL244562 Ki = 29.7 nM 7.53
CHEMBL110365 Ki = 34.0 nM 7.47
CHEMBL244990 Ki = 34.3 nM 7.46
CHEMBL242644 Ki = 36.2 nM 7.44
CHEMBL231156 Ki = 59.0 nM 7.23
CHEMBL244774 Ki = 60.6 nM 7.22
CHEMBL244989 Ki = 71.8 nM 7.14
CHEMBL180010 Ki = 85.4 nM 7.07
CHEMBL244773 Ki = 92.0 nM 7.04
CHEMBL242434 Ki = 117.0 nM 6.93
CHEMBL398175 Ki = 309.0 nM 6.51
CHEMBL244775 Ki = 666.0 nM 6.18
CHEMBL304605 Ki = 941.0 nM 6.03
CHEMBL394863 Ki = 982.0 nM 6.01
CHEMBL396024 Ki = 1810.0 nM 5.74
CHEMBL300780 Ki = 2040.0 nM 5.69