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Assay Detail

CHEMBL1664314

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Binding
Inhibition of human DPP4
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Dipeptidyl peptidase 4 (CHEMBL284)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV.
Zhang Z, Wallace MB, Feng J, Stafford JA, Skene RJ, Shi L, Lee B, Aertgeerts K, Jennings A, Xu R, Kassel DB, Kaldor SW, Navre M, Webb DR, Gwaltney SL.
J Med Chem (2011) 54 : 510 -524
PubMed 21186796 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 49 7.48 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1650430 1 8.52
CHEMBL1650435 1 8.40
CHEMBL1650443 TRELAGLIPTIN 4.0 1 8.40
CHEMBL1650411 1 8.40
CHEMBL1235761 1 8.30
CHEMBL1650423 1 8.30
CHEMBL1650420 1 8.30
CHEMBL1650422 1 8.30
CHEMBL1650434 1 8.22
CHEMBL1650404 1 8.22
CHEMBL1650408 1 8.22
CHEMBL1650429 1 8.22
CHEMBL1650405 1 8.15
CHEMBL376359 ALOGLIPTIN 4.0 1 8.15
CHEMBL1650440 1 8.10
CHEMBL1650432 1 8.10
CHEMBL1650433 1 8.10
CHEMBL1650426 1 8.10
CHEMBL1650406 1 8.10
CHEMBL1650449 1 8.00
CHEMBL1650409 1 8.00
CHEMBL1650418 1 7.92
CHEMBL1650439 1 7.92
CHEMBL1650413 1 7.89
CHEMBL1650403 1 7.85
CHEMBL1650441 1 7.85
CHEMBL1650410 1 7.77
CHEMBL1650424 1 7.70
CHEMBL1650428 1 7.68
CHEMBL1650427 1 7.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1650430 IC50 = 3.0 nM 8.52
CHEMBL1650435 IC50 = 4.0 nM 8.40
CHEMBL1650411 IC50 = 4.0 nM 8.40
CHEMBL1650443 TRELAGLIPTIN IC50 = 4.0 nM 8.40
CHEMBL1235761 IC50 = 5.0 nM 8.30
CHEMBL1650423 IC50 = 5.0 nM 8.30
CHEMBL1650420 IC50 = 5.0 nM 8.30
CHEMBL1650422 IC50 = 5.0 nM 8.30
CHEMBL1650434 IC50 = 6.0 nM 8.22
CHEMBL1650429 IC50 = 6.0 nM 8.22
CHEMBL1650408 IC50 = 6.0 nM 8.22
CHEMBL1650404 IC50 = 6.0 nM 8.22
CHEMBL1650405 IC50 = 7.0 nM 8.15
CHEMBL376359 ALOGLIPTIN IC50 = 7.0 nM 8.15
CHEMBL1650406 IC50 = 8.0 nM 8.10
CHEMBL1650440 IC50 = 8.0 nM 8.10
CHEMBL1650433 IC50 = 8.0 nM 8.10
CHEMBL1650426 IC50 = 8.0 nM 8.10
CHEMBL1650432 IC50 = 8.0 nM 8.10
CHEMBL1650449 IC50 = 10.0 nM 8.00
CHEMBL1650409 IC50 = 10.0 nM 8.00
CHEMBL1650418 IC50 = 12.0 nM 7.92
CHEMBL1650439 IC50 = 12.0 nM 7.92
CHEMBL1650413 IC50 = 13.0 nM 7.89
CHEMBL1650403 IC50 = 14.0 nM 7.85
CHEMBL1650441 IC50 = 14.0 nM 7.85
CHEMBL1650410 IC50 = 17.0 nM 7.77
CHEMBL1650424 IC50 = 20.0 nM 7.70
CHEMBL1650428 IC50 = 21.0 nM 7.68
CHEMBL1650427 IC50 = 22.0 nM 7.66
CHEMBL1650414 IC50 = 23.0 nM 7.64
CHEMBL1650412 IC50 = 23.0 nM 7.64
CHEMBL1650444 IC50 = 27.0 nM 7.57
CHEMBL1650438 IC50 = 36.0 nM 7.44
CHEMBL1650436 IC50 = 57.0 nM 7.24
CHEMBL1650437 IC50 = 68.0 nM 7.17
CHEMBL1650419 IC50 = 77.0 nM 7.11
CHEMBL1650421 IC50 = 200.0 nM 6.70
CHEMBL1650416 IC50 = 240.0 nM 6.62
CHEMBL1650431 IC50 = 430.0 nM 6.37
CHEMBL1650415 IC50 = 540.0 nM 6.27
CHEMBL1650425 IC50 = 570.0 nM 6.24
CHEMBL1650447 IC50 = 590.0 nM 6.23
CHEMBL1650445 IC50 = 830.0 nM 6.08
CHEMBL1650442 IC50 = 890.0 nM 6.05
CHEMBL1650417 IC50 = 990.0 nM 6.00
CHEMBL1650448 IC50 = 3800.0 nM 5.42
CHEMBL1650407 IC50 = 7400.0 nM 5.13
CHEMBL1650446 IC50 = 17000.0 nM 4.77