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Assay Detail

CHEMBL1949347

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

Binding
Displacement of [3H]8-OH-DPAT from 5HT1A receptor in cerebral cortex homogenates after 15 mins
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Cerebral cortex
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Synthesis, in vitro binding studies and docking of long-chain arylpiperazine nitroquipazine analogues, as potential serotonin transporter inhibitors.
Jarończyk M, Wołosewicz K, Gabrielsen M, Nowak G, Kufareva I, Mazurek AP, Ravna AW, Abagyan R, Bojarski AJ, Sylte I, Chilmonczyk Z.
Eur J Med Chem (2012) 49 : 200 -210
PubMed 22309909 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 6.55 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL297702 1 7.96
CHEMBL485540 1 7.89
CHEMBL1945686 1 7.82
CHEMBL485542 1 7.62
CHEMBL485541 1 7.43
CHEMBL299638 1 7.41
CHEMBL483176 1 7.41
CHEMBL1945681 1 6.66
CHEMBL18772 QUIPAZINE 2.0 1 6.64
CHEMBL520024 1 6.56
CHEMBL1945475 1 6.15
CHEMBL1945679 1 6.11
CHEMBL1945680 1 5.96
CHEMBL1945684 1 5.85
CHEMBL1945682 1 5.68
CHEMBL1945685 1 5.50
CHEMBL1945678 1 4.97
CHEMBL1945683 1 4.23
CHEMBL41140 6-NITROQUIPAZINE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL297702 Ki = 11.0 nM 7.96
CHEMBL485540 Ki = 13.0 nM 7.89
CHEMBL1945686 Ki = 15.0 nM 7.82
CHEMBL485542 Ki = 24.0 nM 7.62
CHEMBL485541 Ki = 37.0 nM 7.43
CHEMBL299638 Ki = 39.0 nM 7.41
CHEMBL483176 Ki = 39.0 nM 7.41
CHEMBL1945681 Ki = 221.0 nM 6.66
CHEMBL18772 QUIPAZINE Ki = 230.0 nM 6.64
CHEMBL520024 Ki = 275.0 nM 6.56
CHEMBL1945475 Ki = 711.0 nM 6.15
CHEMBL1945679 Ki = 776.5 nM 6.11
CHEMBL1945680 Ki = 1100.0 nM 5.96
CHEMBL1945684 Ki = 1400.0 nM 5.85
CHEMBL1945682 Ki = 2100.0 nM 5.68
CHEMBL1945685 Ki = 3200.0 nM 5.50
CHEMBL1945678 Ki = 10600.0 nM 4.97
CHEMBL1945683 Ki = 59000.0 nM 4.23
CHEMBL41140 6-NITROQUIPAZINE Ki - -