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Assay Detail

CHEMBL5360446

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Functional
Agonist activity at human 5-HT2A receptor expressed in CHO cells measured after 140 secs by Fluo-4 dye based calcium mobilization assay
ChEMBL ↗
31
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Evaluation of the Indazole Analogs of 5-MeO-DMT and Related Tryptamines as Serotonin Receptor 2 Agonists.
Jayakodiarachchi N, Maurer MA, Schultz DC, Dodd CJ, Thompson Gray A, Cho HP, Boutaud O, Jones CK, Lindsley CW, Bender AM.
ACS Med Chem Lett (2024) 15 : 302 -309
PubMed 38352850 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 31 6.39 8.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL7257 MEBUFOTENIN 2.0 2 8.73
CHEMBL5399968 — — 1 7.38
CHEMBL5424175 — — 2 6.72
CHEMBL5406172 — — 2 6.49
CHEMBL5404610 — — 2 6.49
CHEMBL5434434 — — 2 6.27
CHEMBL5425772 — — 2 5.66
CHEMBL5405688 — — 2 5.64
CHEMBL5437030 — — 2 5.54
CHEMBL5439312 — — 2 5.49
CHEMBL5438716 — — 2 -
CHEMBL5429252 — — 2 -
CHEMBL5429912 — — 2 -
CHEMBL5394562 — — 2 -
CHEMBL5422659 — — 2 -
CHEMBL5401685 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL7257 MEBUFOTENIN EC50 = 1.85 nM 8.73
CHEMBL7257 MEBUFOTENIN EC50 = 2.239 nM 8.65
CHEMBL5399968 — EC50 = 41.3 nM 7.38
CHEMBL5424175 — EC50 = 190.55 nM 6.72
CHEMBL5424175 — EC50 = 189.0 nM 6.72
CHEMBL5406172 — EC50 = 323.59 nM 6.49
CHEMBL5404610 — EC50 = 323.59 nM 6.49
CHEMBL5406172 — EC50 = 325.0 nM 6.49
CHEMBL5404610 — EC50 = 326.0 nM 6.49
CHEMBL5434434 — EC50 = 537.03 nM 6.27
CHEMBL5434434 — EC50 = 537.0 nM 6.27
CHEMBL5425772 — EC50 = 2187.76 nM 5.66
CHEMBL5425772 — EC50 = 2204.0 nM 5.66
CHEMBL5405688 — EC50 = 2290.87 nM 5.64
CHEMBL5405688 — EC50 = 2312.0 nM 5.64
CHEMBL5437030 — EC50 = 2852.0 nM 5.54
CHEMBL5437030 — EC50 = 2884.03 nM 5.54
CHEMBL5439312 — EC50 = 3235.94 nM 5.49
CHEMBL5439312 — EC50 = 3228.0 nM 5.49
CHEMBL5394562 — EC50 > 10000.0 nM -
CHEMBL5422659 — EC50 > 10000.0 nM -
CHEMBL5401685 — EC50 > 10000.0 nM -
CHEMBL5429912 — EC50 > 10000.0 nM -
CHEMBL5429252 — EC50 > 10000.0 nM -
CHEMBL5438716 — EC50 > 10000.0 nM -
CHEMBL5401685 — EC50 > 10000.0 nM -
CHEMBL5422659 — EC50 > 10000.0 nM -
CHEMBL5394562 — EC50 > 10000.0 nM -
CHEMBL5429912 — EC50 > 10000.0 nM -
CHEMBL5429252 — EC50 > 10000.0 nM -
CHEMBL5438716 — EC50 > 10000.0 nM -