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Assay Detail

CHEMBL616594

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

Binding
Binding affinity against 5-hydroxytryptamine 1A receptor from CHO-K1 cells, using [3H]8-OH-DPAT as the radioligand.
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO-K1
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 1A (CHEMBL273)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Structure-activity relationships in the 8-amino-6,7,8,9-tetrahydro-3H-benz[e]indole ring system. 1. Effects of substituents in the aromatic system on serotonin and dopamine receptor subtypes.
Stjernlöf P, Ennis MD, Hansson LO, Hoffman RL, Ghazal NB, Sundell S, Smith MW, Svensson K, Carlsson A, Wikström H.
J Med Chem (1995) 38 : 2202 -2216
PubMed 7783152 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 38 8.30 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL307786 1 9.70
CHEMBL304426 1 9.70
CHEMBL71625 1 9.70
CHEMBL71176 1 9.52
CHEMBL70589 1 9.40
CHEMBL71804 1 9.30
CHEMBL56 8-OH-DPAT 1 9.30
CHEMBL441256 1 9.30
CHEMBL70652 1 9.10
CHEMBL308347 1 9.10
CHEMBL302171 1 8.85
CHEMBL305743 1 8.85
CHEMBL70710 1 8.82
CHEMBL303021 1 8.70
CHEMBL71474 1 8.64
CHEMBL65196 1 8.48
CHEMBL304573 1 8.43
CHEMBL302172 1 8.28
CHEMBL70985 1 8.15
CHEMBL71139 1 8.14
CHEMBL302994 1 8.07
CHEMBL71663 1 7.96
CHEMBL303269 1 7.96
CHEMBL306869 1 7.89
CHEMBL69562 1 7.89
CHEMBL71395 1 7.85
CHEMBL71091 1 7.85
CHEMBL71247 1 7.77
CHEMBL71899 1 7.75
CHEMBL302263 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL307786 Ki = 0.2 nM 9.70
CHEMBL71625 Ki = 0.2 nM 9.70
CHEMBL304426 Ki = 0.2 nM 9.70
CHEMBL71176 Ki = 0.3 nM 9.52
CHEMBL70589 Ki = 0.4 nM 9.40
CHEMBL71804 Ki = 0.5 nM 9.30
CHEMBL56 8-OH-DPAT Ki = 0.5 nM 9.30
CHEMBL441256 Ki = 0.5 nM 9.30
CHEMBL70652 Ki = 0.8 nM 9.10
CHEMBL308347 Ki = 0.8 nM 9.10
CHEMBL305743 Ki = 1.4 nM 8.85
CHEMBL302171 Ki = 1.4 nM 8.85
CHEMBL70710 Ki = 1.5 nM 8.82
CHEMBL303021 Ki = 2.0 nM 8.70
CHEMBL71474 Ki = 2.3 nM 8.64
CHEMBL65196 Ki = 3.3 nM 8.48
CHEMBL304573 Ki = 3.7 nM 8.43
CHEMBL302172 Ki = 5.2 nM 8.28
CHEMBL70985 Ki = 7.1 nM 8.15
CHEMBL71139 Ki = 7.3 nM 8.14
CHEMBL302994 Ki = 8.6 nM 8.07
CHEMBL71663 Ki = 11.0 nM 7.96
CHEMBL303269 Ki = 11.0 nM 7.96
CHEMBL306869 Ki = 13.0 nM 7.89
CHEMBL69562 Ki = 13.0 nM 7.89
CHEMBL71395 Ki = 14.0 nM 7.85
CHEMBL71091 Ki = 14.0 nM 7.85
CHEMBL71247 Ki = 17.0 nM 7.77
CHEMBL71899 Ki = 18.0 nM 7.75
CHEMBL302263 Ki = 20.0 nM 7.70
CHEMBL70431 Ki = 24.0 nM 7.62
CHEMBL71319 Ki = 28.0 nM 7.55
CHEMBL71299 Ki = 40.0 nM 7.40
CHEMBL307521 Ki = 49.0 nM 7.31
CHEMBL71454 Ki = 113.0 nM 6.95
CHEMBL71676 Ki = 123.0 nM 6.91
CHEMBL302373 Ki = 134.0 nM 6.87
CHEMBL70882 Ki = 250.0 nM 6.60