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Assay Detail

CHEMBL615779

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

Binding
Binding affinity was measured on cloned Human 5-hydroxytryptamine 1A receptor which is labeled by [3H]8-OH-DPAT
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Derivatives of (R)-1,11-methyleneaporphine: synthesis, structure, and interactions with G-protein coupled receptors.
Linnanen T, Brisander M, Unelius L, Sundholm G, Hacksell U, Johansson AM.
J Med Chem (2000) 43 : 1339 -1349
PubMed 10753471 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.58 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL26998 1 8.89
CHEMBL282863 1 8.30
CHEMBL27940 1 7.84
CHEMBL27132 1 7.51
CHEMBL284586 1 7.39
CHEMBL281357 1 7.10
CHEMBL22778 1 7.06
CHEMBL53 APOMORPHINE 4.0 1 6.53
CHEMBL18840 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL26998 Ki = 1.3 nM 8.89
CHEMBL282863 Ki = 5.05 nM 8.30
CHEMBL27940 Ki = 14.4 nM 7.84
CHEMBL27132 Ki = 31.1 nM 7.51
CHEMBL284586 Ki = 40.7 nM 7.39
CHEMBL281357 Ki = 80.0 nM 7.10
CHEMBL22778 Ki = 87.0 nM 7.06
CHEMBL53 APOMORPHINE Ki = 296.0 nM 6.53
CHEMBL18840 Ki < 0.3 nM -