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Assay Detail

CHEMBL1060393

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 CHO cells
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis, potency, and in vivo evaluation of 2-piperazin-1-ylquinoline analogues as dual serotonin reuptake inhibitors and serotonin 5-HT1A receptor antagonists.
Zhou D, Stack GP, Lo J, Failli AA, Evrard DA, Harrison BL, Hatzenbuhler NT, Tran M, Croce S, Yi S, Golembieski J, Hornby GA, Lai M, Lin Q, Schechter LE, Smith DL, Shilling AD, Huselton C, Mitchell P, Beyer CE, Andree TH.
J Med Chem (2009) 52 : 4955 -4959
PubMed 19719241 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 7.95 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL31354 WAY-100,635 1 9.05
CHEMBL551909 1 8.82
CHEMBL564148 1 8.70
CHEMBL560170 1 8.55
CHEMBL562248 1 8.52
CHEMBL551964 1 8.43
CHEMBL551107 1 8.26
CHEMBL551304 1 8.17
CHEMBL559778 1 8.14
CHEMBL550700 1 7.76
CHEMBL556474 1 7.70
CHEMBL550169 1 7.48
CHEMBL550576 1 7.33
CHEMBL565234 1 6.78
CHEMBL551105 1 6.76
CHEMBL559579 1 6.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL31354 WAY-100,635 Ki = 0.9 nM 9.05
CHEMBL551909 Ki = 1.5 nM 8.82
CHEMBL564148 Ki = 2.0 nM 8.70
CHEMBL560170 Ki = 2.8 nM 8.55
CHEMBL562248 Ki = 3.02 nM 8.52
CHEMBL551964 Ki = 3.7 nM 8.43
CHEMBL551107 Ki = 5.5 nM 8.26
CHEMBL551304 Ki = 6.8 nM 8.17
CHEMBL559778 Ki = 7.2 nM 8.14
CHEMBL550700 Ki = 17.2 nM 7.76
CHEMBL556474 Ki = 20.0 nM 7.70
CHEMBL550169 Ki = 32.9 nM 7.48
CHEMBL550576 Ki = 47.3 nM 7.33
CHEMBL565234 Ki = 167.0 nM 6.78
CHEMBL551105 Ki = 172.0 nM 6.76
CHEMBL559579 Ki = 214.1 nM 6.67