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Assay Detail

CHEMBL4670405

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

Functional
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of Novel pERK1/2- or β-Arrestin-Preferring 5-HT Receptor-Biased Agonists: Diversified Therapeutic-like versus Side Effect Profile.
Sniecikowska J,Gluch-Lutwin M,Bucki A,Więckowska A,Siwek A,Jastrzebska-Wiesek M,Partyka A,Wilczyńska D,Pytka K,Latacz G,Przejczowska-Pomierny K,Wyska E,Wesołowska A,Pawłowski M,Newman-Tancredi A,Kolaczkowski M
J Med Chem (2020) 63 : 10946 -10971
PubMed 32883072 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 30 8.19 10.88

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4757755 1 10.88
CHEMBL4755058 1 10.86
CHEMBL4752177 1 10.18
CHEMBL4756233 1 10.06
CHEMBL4796345 1 9.95
CHEMBL4751777 1 9.86
CHEMBL4756041 1 9.47
CHEMBL4777581 1 9.18
CHEMBL4786067 1 8.98
CHEMBL4750444 1 8.22
CHEMBL4790600 1 8.18
CHEMBL4741857 1 8.09
CHEMBL4760621 1 7.83
CHEMBL4781985 1 7.82
CHEMBL4739908 1 7.80
CHEMBL4760666 1 7.77
CHEMBL4760271 1 7.74
CHEMBL4797282 1 7.71
CHEMBL4790662 1 7.69
CHEMBL4746386 1 7.59
CHEMBL39 SEROTONIN 3.0 1 7.51
CHEMBL56 8-OH-DPAT 1 7.50
CHEMBL4752833 1 7.40
CHEMBL4747425 1 7.37
CHEMBL230963 1 7.22
CHEMBL49 BUSPIRONE 4.0 1 7.14
CHEMBL4740430 1 6.56
CHEMBL4753394 1 6.48
CHEMBL4797752 1 6.32
CHEMBL4747083 1 6.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4757755 EC50 = 0.01318 nM 10.88
CHEMBL4755058 EC50 = 0.0138 nM 10.86
CHEMBL4752177 EC50 = 0.06607 nM 10.18
CHEMBL4756233 EC50 = 0.0871 nM 10.06
CHEMBL4796345 EC50 = 0.1122 nM 9.95
CHEMBL4751777 EC50 = 0.138 nM 9.86
CHEMBL4756041 EC50 = 0.3388 nM 9.47
CHEMBL4777581 EC50 = 0.6607 nM 9.18
CHEMBL4786067 EC50 = 1.047 nM 8.98
CHEMBL4750444 EC50 = 6.026 nM 8.22
CHEMBL4790600 EC50 = 6.607 nM 8.18
CHEMBL4741857 EC50 = 8.128 nM 8.09
CHEMBL4760621 EC50 = 14.79 nM 7.83
CHEMBL4781985 EC50 = 15.14 nM 7.82
CHEMBL4739908 EC50 = 15.85 nM 7.80
CHEMBL4760666 EC50 = 16.98 nM 7.77
CHEMBL4760271 EC50 = 18.2 nM 7.74
CHEMBL4797282 EC50 = 19.5 nM 7.71
CHEMBL4790662 EC50 = 20.42 nM 7.69
CHEMBL4746386 EC50 = 25.7 nM 7.59
CHEMBL39 SEROTONIN EC50 = 30.9 nM 7.51
CHEMBL56 8-OH-DPAT EC50 = 31.62 nM 7.50
CHEMBL4752833 EC50 = 39.81 nM 7.40
CHEMBL4747425 EC50 = 42.66 nM 7.37
CHEMBL230963 EC50 = 60.26 nM 7.22
CHEMBL49 BUSPIRONE EC50 = 72.44 nM 7.14
CHEMBL4740430 EC50 = 275.42 nM 6.56
CHEMBL4753394 EC50 = 331.13 nM 6.48
CHEMBL4797752 EC50 = 478.63 nM 6.32
CHEMBL4747083 EC50 = 562.34 nM 6.25