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Assay Detail

CHEMBL2061652

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Functional
Agonist activity against S1P1 receptor by cell based FRET assay
ChEMBL ↗
50
Total Activities
50
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

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

Publication

Discovery of novel 1,2,4-thiadiazole derivatives as potent, orally active agonists of sphingosine 1-phosphate receptor subtype 1 (S1P(1)).
Ren F, Deng G, Wang H, Luan L, Meng Q, Xu Q, Xu H, Xu X, Zhang H, Zhao B, Li C, Guo TB, Yang J, Zhang W, Zhao Y, Jia Q, Lu H, Xiang JN, Elliott JD, Lin X.
J Med Chem (2012) 55 : 4286 -4296
PubMed 22500954 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 50 8.23 10.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2059683 — — 1 10.80
CHEMBL2059684 — — 1 10.70
CHEMBL2059687 — — 1 10.00
CHEMBL2057282 — — 1 9.80
CHEMBL2059515 — — 1 9.70
CHEMBL2059686 — — 1 9.60
CHEMBL2057283 — — 1 9.60
CHEMBL2059688 — — 1 9.60
CHEMBL2057286 — — 1 9.10
CHEMBL2057285 — — 1 9.10
CHEMBL2057232 — — 1 9.00
CHEMBL2059516 — — 1 8.90
CHEMBL2059671 — — 1 8.90
CHEMBL2059518 — — 1 8.90
CHEMBL2059527 — — 1 8.80
CHEMBL2059675 — — 1 8.70
CHEMBL2059670 — — 1 8.70
CHEMBL2059517 — — 1 8.60
CHEMBL2059520 — — 1 8.50
CHEMBL2059519 — — 1 8.50
CHEMBL2059689 — — 1 8.40
CHEMBL2059521 — — 1 8.40
CHEMBL2059669 — — 1 8.40
CHEMBL2059676 — — 1 8.30
CHEMBL2059672 — — 1 8.30
CHEMBL2059522 — — 1 8.30
CHEMBL2057284 — — 1 8.10
CHEMBL2059681 — — 1 8.00
CHEMBL2059685 — — 1 7.80
CHEMBL2059528 — — 1 7.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2059683 — EC50 = 0.01585 nM 10.80
CHEMBL2059684 — EC50 = 0.01995 nM 10.70
CHEMBL2059687 — EC50 = 0.1 nM 10.00
CHEMBL2057282 — EC50 = 0.1585 nM 9.80
CHEMBL2059515 — EC50 = 0.1995 nM 9.70
CHEMBL2059686 — EC50 = 0.2512 nM 9.60
CHEMBL2057283 — EC50 = 0.2512 nM 9.60
CHEMBL2059688 — EC50 = 0.2512 nM 9.60
CHEMBL2057286 — EC50 = 0.7943 nM 9.10
CHEMBL2057285 — EC50 = 0.7943 nM 9.10
CHEMBL2057232 — EC50 = 1.0 nM 9.00
CHEMBL2059518 — EC50 = 1.259 nM 8.90
CHEMBL2059671 — EC50 = 1.259 nM 8.90
CHEMBL2059516 — EC50 = 1.259 nM 8.90
CHEMBL2059527 — EC50 = 1.585 nM 8.80
CHEMBL2059675 — EC50 = 1.995 nM 8.70
CHEMBL2059670 — EC50 = 1.995 nM 8.70
CHEMBL2059517 — EC50 = 2.512 nM 8.60
CHEMBL2059520 — EC50 = 3.162 nM 8.50
CHEMBL2059519 — EC50 = 3.162 nM 8.50
CHEMBL2059689 — EC50 = 3.981 nM 8.40
CHEMBL2059521 — EC50 = 3.981 nM 8.40
CHEMBL2059669 — EC50 = 3.981 nM 8.40
CHEMBL2059522 — EC50 = 5.012 nM 8.30
CHEMBL2059676 — EC50 = 5.012 nM 8.30
CHEMBL2059672 — EC50 = 5.012 nM 8.30
CHEMBL2057284 — EC50 = 7.943 nM 8.10
CHEMBL2059681 — EC50 = 10.0 nM 8.00
CHEMBL2059685 — EC50 = 15.85 nM 7.80
CHEMBL2059528 — EC50 = 25.12 nM 7.60
CHEMBL2059677 — EC50 = 25.12 nM 7.60
CHEMBL2059529 — EC50 = 31.62 nM 7.50
CHEMBL2059663 — EC50 = 31.62 nM 7.50
CHEMBL2059682 — EC50 = 100.0 nM 7.00
CHEMBL2059674 — EC50 = 125.89 nM 6.90
CHEMBL2059680 — EC50 = 158.49 nM 6.80
CHEMBL2057287 — EC50 = 199.53 nM 6.70
CHEMBL2059678 — EC50 = 251.19 nM 6.60
CHEMBL2059679 — EC50 = 398.11 nM 6.40
CHEMBL2059664 — EC50 = 630.96 nM 6.20
CHEMBL2059523 — EC50 = 630.96 nM 6.20
CHEMBL2057288 — EC50 = 1584.89 nM 5.80
CHEMBL2059524 — EC50 = 2511.89 nM 5.60
CHEMBL2059526 — EC50 > 10000.0 nM -
CHEMBL2059525 — EC50 > 10000.0 nM -
CHEMBL2059665 — EC50 > 3162.28 nM -
CHEMBL2059666 — EC50 > 3162.28 nM -
CHEMBL2059667 — EC50 > 3162.28 nM -
CHEMBL2059673 — EC50 > 3162.28 nM -
CHEMBL2059668 — EC50 > 3162.28 nM -