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Assay Detail

CHEMBL4628378

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Binding
Binding affinity to human 5HT1A receptor
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Identification of C10 nitrogen-containing aporphines with dopamine D<sub>1</sub> versus D<sub>5</sub> receptor selectivity.
Karki A, Juarez R, Namballa HK, Alberts I, Harding WW.
Bioorg Med Chem Lett (2020) 30 : 127053 -127053
PubMed 32107165 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 6.76 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56 8-OH-DPAT 1 9.10
CHEMBL4633015 1 7.08
CHEMBL4632693 1 7.03
CHEMBL4636242 1 7.00
CHEMBL4639398 1 6.81
CHEMBL4638749 1 6.69
CHEMBL4634039 1 6.57
CHEMBL4643500 1 6.46
CHEMBL4636589 1 6.37
CHEMBL4638378 1 6.36
CHEMBL4646927 1 6.34
CHEMBL4636948 1 6.26
CHEMBL4645124 1 5.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56 8-OH-DPAT Ki = 0.8 nM 9.10
CHEMBL4633015 Ki = 83.0 nM 7.08
CHEMBL4632693 Ki = 93.0 nM 7.03
CHEMBL4636242 Ki = 100.0 nM 7.00
CHEMBL4639398 Ki = 156.0 nM 6.81
CHEMBL4638749 Ki = 206.0 nM 6.69
CHEMBL4634039 Ki = 269.0 nM 6.57
CHEMBL4643500 Ki = 350.0 nM 6.46
CHEMBL4636589 Ki = 428.0 nM 6.37
CHEMBL4638378 Ki = 439.0 nM 6.36
CHEMBL4646927 Ki = 458.0 nM 6.34
CHEMBL4636948 Ki = 548.0 nM 6.26
CHEMBL4645124 Ki = 1676.0 nM 5.78