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Assay Detail

CHEMBL616591

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

Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1A receptor expressed in CHO cells, by using [3H]8-OH-DPAT as radioligand.
ChEMBL ↗
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
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. 2. Effects of 8-amino nitrogen substitution on serotonin receptor binding and pharmacology.
Ennis MD, Stjernlöf P, Hoffman RL, Ghazal NB, Smith MW, Svensson K, Wikström H, Haadsma-Svensson SR, Lin CH.
J Med Chem (1995) 38 : 2217 -2230
PubMed 7783153 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 45 8.81 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL304767 — — 1 10.40
CHEMBL308934 — — 1 10.15
CHEMBL72062 — — 1 10.00
CHEMBL307786 — — 1 9.70
CHEMBL1788200 — — 1 9.70
CHEMBL71625 — — 1 9.70
CHEMBL304426 — — 1 9.70
CHEMBL306198 — — 1 9.62
CHEMBL304984 — — 1 9.52
CHEMBL71145 — — 1 9.22
CHEMBL70680 — — 1 9.22
CHEMBL1788198 — — 1 9.22
CHEMBL71640 — — 1 9.22
CHEMBL71469 — — 1 9.15
CHEMBL72285 — — 1 9.15
CHEMBL303921 — — 1 9.10
CHEMBL69560 — — 1 9.10
CHEMBL312525 — — 1 9.00
CHEMBL1744039 — — 1 8.96
CHEMBL305837 — — 1 8.92
CHEMBL302171 — — 1 8.85
CHEMBL2112317 — — 1 8.82
CHEMBL1744040 — — 1 8.82
CHEMBL70606 — — 1 8.72
CHEMBL69943 — — 1 8.72
CHEMBL69729 — — 1 8.60
CHEMBL420191 — — 1 8.57
CHEMBL423127 — — 1 8.55
CHEMBL306197 — — 1 8.54
CHEMBL305976 — — 1 8.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL304767 — Ki = 0.04 nM 10.40
CHEMBL308934 — Ki = 0.07 nM 10.15
CHEMBL72062 — Ki = 0.1 nM 10.00
CHEMBL307786 — Ki = 0.2 nM 9.70
CHEMBL1788200 — Ki = 0.2 nM 9.70
CHEMBL71625 — Ki = 0.2 nM 9.70
CHEMBL304426 — Ki = 0.2 nM 9.70
CHEMBL306198 — Ki = 0.24 nM 9.62
CHEMBL304984 — Ki = 0.3 nM 9.52
CHEMBL71640 — Ki = 0.6 nM 9.22
CHEMBL1788198 — Ki = 0.6 nM 9.22
CHEMBL70680 — Ki = 0.6 nM 9.22
CHEMBL71145 — Ki = 0.6 nM 9.22
CHEMBL71469 — Ki = 0.7 nM 9.15
CHEMBL72285 — Ki = 0.7 nM 9.15
CHEMBL303921 — Ki = 0.8 nM 9.10
CHEMBL69560 — Ki = 0.8 nM 9.10
CHEMBL312525 — Ki = 1.0 nM 9.00
CHEMBL1744039 — Ki = 1.1 nM 8.96
CHEMBL305837 — Ki = 1.2 nM 8.92
CHEMBL302171 — Ki = 1.4 nM 8.85
CHEMBL1744040 — Ki = 1.5 nM 8.82
CHEMBL2112317 — Ki = 1.5 nM 8.82
CHEMBL70606 — Ki = 1.9 nM 8.72
CHEMBL69943 — Ki = 1.9 nM 8.72
CHEMBL69729 — Ki = 2.5 nM 8.60
CHEMBL420191 — Ki = 2.7 nM 8.57
CHEMBL423127 — Ki = 2.8 nM 8.55
CHEMBL306197 — Ki = 2.9 nM 8.54
CHEMBL305976 — Ki = 3.2 nM 8.49
CHEMBL65196 — Ki = 3.3 nM 8.48
CHEMBL70980 — Ki = 3.4 nM 8.47
CHEMBL1744041 — Ki = 3.6 nM 8.44
CHEMBL309121 — Ki = 4.6 nM 8.34
CHEMBL302172 — Ki = 5.2 nM 8.28
CHEMBL420748 — Ki = 12.0 nM 7.92
CHEMBL71409 — Ki = 14.0 nM 7.85
CHEMBL73112 — Ki = 15.0 nM 7.82
CHEMBL413105 — Ki = 15.0 nM 7.82
CHEMBL303339 — Ki = 15.0 nM 7.82
CHEMBL1788196 — Ki = 18.0 nM 7.75
CHEMBL70970 — Ki = 42.0 nM 7.38
CHEMBL292274 — Ki = 137.0 nM 6.86
CHEMBL70489 — Ki > 200.0 nM -
CHEMBL1788197 — Ki < 0.02 nM -