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Assay Detail

CHEMBL3377152

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Functional
Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 2A (CHEMBL224)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Alpha-ethyltryptamines as dual dopamine-serotonin releasers.
Blough BE, Landavazo A, Partilla JS, Decker AM, Page KM, Baumann MH, Rothman RB.
Bioorg Med Chem Lett (2014) 24 : 4754 -4758
PubMed 25193229 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 26 7.54 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8165 5-METHOXYTRYPTAMINE 1 9.30
CHEMBL275628 1 8.58
CHEMBL1288716 1 8.39
CHEMBL381160 1 8.34
CHEMBL1288717 1 8.29
CHEMBL331241 1 8.22
CHEMBL1906905 1 8.20
CHEMBL6640 TRYPTAMINE 1 8.13
CHEMBL96816 1 8.07
CHEMBL343529 1 8.04
CHEMBL3330643 1 7.73
CHEMBL30713 1 7.64
CHEMBL382635 1 7.55
CHEMBL3330640 1 7.42
CHEMBL204839 1 7.35
CHEMBL348588 1 7.29
CHEMBL3330642 1 7.12
CHEMBL3330641 1 6.68
CHEMBL3330648 1 6.61
CHEMBL3330647 1 6.60
CHEMBL3330644 1 6.30
CHEMBL3330646 1 5.90
CHEMBL337825 1 5.61
CHEMBL1619758 ETRYPTAMINE 2.0 1 -
CHEMBL3330645 1 -
CHEMBL471839 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8165 5-METHOXYTRYPTAMINE EC50 = 0.503 nM 9.30
CHEMBL275628 EC50 = 2.64 nM 8.58
CHEMBL1288716 EC50 = 4.11 nM 8.39
CHEMBL381160 EC50 = 4.56 nM 8.34
CHEMBL1288717 EC50 = 5.14 nM 8.29
CHEMBL331241 EC50 = 6.0 nM 8.22
CHEMBL1906905 EC50 = 6.27 nM 8.20
CHEMBL6640 TRYPTAMINE EC50 = 7.36 nM 8.13
CHEMBL96816 EC50 = 8.47 nM 8.07
CHEMBL343529 EC50 = 9.02 nM 8.04
CHEMBL3330643 EC50 = 18.8 nM 7.73
CHEMBL30713 EC50 = 23.1 nM 7.64
CHEMBL382635 EC50 = 28.1 nM 7.55
CHEMBL3330640 EC50 = 38.3 nM 7.42
CHEMBL204839 EC50 = 44.7 nM 7.35
CHEMBL348588 EC50 = 50.7 nM 7.29
CHEMBL3330642 EC50 = 75.3 nM 7.12
CHEMBL3330641 EC50 = 209.0 nM 6.68
CHEMBL3330648 EC50 = 246.0 nM 6.61
CHEMBL3330647 EC50 = 249.0 nM 6.60
CHEMBL3330644 EC50 = 496.0 nM 6.30
CHEMBL3330646 EC50 = 1250.0 nM 5.90
CHEMBL337825 EC50 = 2443.0 nM 5.61
CHEMBL1619758 ETRYPTAMINE EC50 > 10000.0 nM -
CHEMBL3330645 EC50 - -
CHEMBL471839 EC50 - -