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Assay Detail

CHEMBL670667

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

Binding
Displacement of [3H]U-86170 from human D2-dopamine receptor expressed in CHO K1 cells
14
Total Activities
14
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 Expert

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel 2-substituted tetrahydro-3H-benz[e]indolamines: highly potent and selective agonists acting at the 5-HT1A receptor as possible anxiolytics and antidepressants.
Romero AG, Leiby JA, McCall RB, Piercey MF, Smith MW, Han F.
J Med Chem (1993) 36 : 2066 -2074
PubMed 8101876 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 6.84 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL49 BUSPIRONE 4.0 1 7.89
CHEMBL71920 U-92,016-A 1 7.46
CHEMBL1744037 1 7.42
CHEMBL1744088 1 7.36
CHEMBL26998 1 7.03
CHEMBL1744036 1 6.67
CHEMBL1788192 1 6.41
CHEMBL1744089 1 6.07
CHEMBL1744035 1 6.05
CHEMBL1788191 1 6.04
CHEMBL1744038 1 -
CHEMBL1788325 1 -
CHEMBL1788190 1 -
CHEMBL1788324 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL49 BUSPIRONE Ki = 13.0 nM 7.89
CHEMBL71920 U-92,016-A Ki = 35.0 nM 7.46
CHEMBL1744037 Ki = 38.0 nM 7.42
CHEMBL1744088 Ki = 44.0 nM 7.36
CHEMBL26998 Ki = 93.0 nM 7.03
CHEMBL1744036 Ki = 215.0 nM 6.67
CHEMBL1788192 Ki = 389.0 nM 6.41
CHEMBL1744089 Ki = 857.0 nM 6.07
CHEMBL1744035 Ki = 896.0 nM 6.05
CHEMBL1788191 Ki = 914.0 nM 6.04
CHEMBL1744038 Ki > 1000.0 nM -
CHEMBL1788325 Ki > 1667.0 nM -
CHEMBL1788190 Ki > 1000.0 nM -
CHEMBL1788324 Ki > 333.0 nM -