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Assay Detail

CHEMBL2020024

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Functional
Agonist activity at S1P1 receptor by Tango assay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Sphingosine 1-phosphate receptor 1 (CHEMBL4333)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Indole-propionic acid derivatives as potent, S1P3-sparing and EAE efficacious sphingosine-1-phosphate 1 (S1P1) receptor agonists.
Meng Q, Zhao B, Xu Q, Xu X, Deng G, Li C, Luan L, Ren F, Wang H, Xu H, Xu Y, Zhang H, Xiang JN, Elliott JD, Guo TB, Zhao Y, Zhang W, Lu H, Lin X.
Bioorg Med Chem Lett (2012) 22 : 2794 -2797
PubMed 22429468 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 31 8.50 10.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2018176 1 10.90
CHEMBL2018320 1 10.50
CHEMBL2018321 1 10.40
CHEMBL2018319 1 10.30
CHEMBL2018322 1 10.10
CHEMBL2018178 1 9.70
CHEMBL2018177 1 9.60
CHEMBL2018306 1 9.60
CHEMBL2018324 1 9.50
CHEMBL2018179 1 9.40
CHEMBL2018318 1 9.40
CHEMBL2018307 1 8.80
CHEMBL2018174 1 8.60
CHEMBL2018309 1 8.50
CHEMBL2018316 1 8.30
CHEMBL2018327 1 8.20
CHEMBL2018326 1 7.70
CHEMBL2018330 1 7.60
CHEMBL2018317 1 7.40
CHEMBL2018308 1 7.00
CHEMBL2018325 1 6.70
CHEMBL2018175 1 6.40
CHEMBL2018312 1 6.40
CHEMBL2018310 1 5.90
CHEMBL2018313 1 5.50
CHEMBL2018315 1 -
CHEMBL2018323 1 -
CHEMBL2018314 1 -
CHEMBL2018311 1 -
CHEMBL2018328 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2018176 EC50 = 0.01259 nM 10.90
CHEMBL2018320 EC50 = 0.03162 nM 10.50
CHEMBL2018321 EC50 = 0.03981 nM 10.40
CHEMBL2018319 EC50 = 0.05012 nM 10.30
CHEMBL2018322 EC50 = 0.07943 nM 10.10
CHEMBL2018178 EC50 = 0.1995 nM 9.70
CHEMBL2018177 EC50 = 0.2512 nM 9.60
CHEMBL2018306 EC50 = 0.2512 nM 9.60
CHEMBL2018324 EC50 = 0.3162 nM 9.50
CHEMBL2018179 EC50 = 0.3981 nM 9.40
CHEMBL2018318 EC50 = 0.3981 nM 9.40
CHEMBL2018307 EC50 = 1.585 nM 8.80
CHEMBL2018174 EC50 = 2.512 nM 8.60
CHEMBL2018309 EC50 = 3.162 nM 8.50
CHEMBL2018316 EC50 = 5.012 nM 8.30
CHEMBL2018327 EC50 = 6.31 nM 8.20
CHEMBL2018326 EC50 = 19.95 nM 7.70
CHEMBL2018330 EC50 = 25.12 nM 7.60
CHEMBL2018317 EC50 = 39.81 nM 7.40
CHEMBL2018308 EC50 = 100.0 nM 7.00
CHEMBL2018325 EC50 = 199.53 nM 6.70
CHEMBL2018175 EC50 = 398.11 nM 6.40
CHEMBL2018312 EC50 = 398.11 nM 6.40
CHEMBL2018310 EC50 = 1258.93 nM 5.90
CHEMBL2018313 EC50 = 3162.28 nM 5.50
CHEMBL2018315 EC50 > 10000.0 nM -
CHEMBL2018323 EC50 = 0.00631 nM -
CHEMBL2018314 EC50 > 10000.0 nM -
CHEMBL2018311 EC50 > 3162.28 nM -
CHEMBL2018328 EC50 < 0.01 nM -
CHEMBL2018329 EC50 < 0.01 nM -