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Assay Detail

CHEMBL3388490

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

Binding
Inhibition of purified His6-tagged recombinant human HPPD assessed as inhibition of maleylacetoacetate formation after 30 mins by UV/visible spectrophotometry
45
Total Activities
45
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

4-hydroxyphenylpyruvate dioxygenase (CHEMBL1861)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pyrazolone-quinazolone hybrids: a novel class of human 4-hydroxyphenylpyruvate dioxygenase inhibitors.
Xu YL, Lin HY, Cao RJ, Ming ZZ, Yang WC, Yang GF.
Bioorg Med Chem (2014) 22 : 5194 -5211
PubMed 25182962 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 45 7.24 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3342603 1 8.00
CHEMBL3343183 1 7.96
CHEMBL3342605 1 7.89
CHEMBL3342604 1 7.85
CHEMBL3342432 1 7.82
CHEMBL3342610 1 7.75
CHEMBL3342431 1 7.72
CHEMBL3342602 1 7.70
CHEMBL3342609 1 7.66
CHEMBL3342598 1 7.66
CHEMBL3342599 1 7.62
CHEMBL3342611 1 7.60
CHEMBL3343184 1 7.60
CHEMBL3342607 1 7.51
CHEMBL3342614 1 7.50
CHEMBL3342608 1 7.47
CHEMBL3342606 1 7.47
CHEMBL1337 NITISINONE 4.0 1 7.43
CHEMBL3342601 1 7.42
CHEMBL3343182 1 7.40
CHEMBL3342600 1 7.24
CHEMBL3343187 1 7.23
CHEMBL3342612 1 7.22
CHEMBL3342416 1 7.13
CHEMBL3342415 1 7.10
CHEMBL3342426 1 7.09
CHEMBL3342412 1 7.07
CHEMBL3342428 1 7.06
CHEMBL3343186 1 7.05
CHEMBL3342419 1 7.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3342603 Ki = 10.0 nM 8.00
CHEMBL3343183 Ki = 11.0 nM 7.96
CHEMBL3342605 Ki = 13.0 nM 7.89
CHEMBL3342604 Ki = 14.0 nM 7.85
CHEMBL3342432 Ki = 15.0 nM 7.82
CHEMBL3342610 Ki = 18.0 nM 7.75
CHEMBL3342431 Ki = 19.0 nM 7.72
CHEMBL3342602 Ki = 20.0 nM 7.70
CHEMBL3342609 Ki = 22.0 nM 7.66
CHEMBL3342598 Ki = 22.0 nM 7.66
CHEMBL3342599 Ki = 24.0 nM 7.62
CHEMBL3343184 Ki = 25.0 nM 7.60
CHEMBL3342611 Ki = 25.0 nM 7.60
CHEMBL3342607 Ki = 31.0 nM 7.51
CHEMBL3342614 Ki = 32.0 nM 7.50
CHEMBL3342608 Ki = 34.0 nM 7.47
CHEMBL3342606 Ki = 34.0 nM 7.47
CHEMBL1337 NITISINONE Ki = 37.0 nM 7.43
CHEMBL3342601 Ki = 38.0 nM 7.42
CHEMBL3343182 Ki = 40.0 nM 7.40
CHEMBL3342600 Ki = 58.0 nM 7.24
CHEMBL3343187 Ki = 59.0 nM 7.23
CHEMBL3342612 Ki = 60.0 nM 7.22
CHEMBL3342416 Ki = 74.0 nM 7.13
CHEMBL3342415 Ki = 79.0 nM 7.10
CHEMBL3342426 Ki = 81.0 nM 7.09
CHEMBL3342412 Ki = 86.0 nM 7.07
CHEMBL3342428 Ki = 87.0 nM 7.06
CHEMBL3343186 Ki = 90.0 nM 7.05
CHEMBL3342419 Ki = 90.0 nM 7.05
CHEMBL3342418 Ki = 93.0 nM 7.03
CHEMBL3342430 Ki = 109.0 nM 6.96
CHEMBL3342422 Ki = 130.0 nM 6.89
CHEMBL3342423 Ki = 156.0 nM 6.81
CHEMBL3342613 Ki = 160.0 nM 6.80
CHEMBL3342425 Ki = 161.0 nM 6.79
CHEMBL3343185 Ki = 170.0 nM 6.77
CHEMBL3342417 Ki = 173.0 nM 6.76
CHEMBL3342429 Ki = 177.0 nM 6.75
CHEMBL3342414 Ki = 207.0 nM 6.68
CHEMBL3342427 Ki = 219.0 nM 6.66
CHEMBL3342421 Ki = 238.0 nM 6.62
CHEMBL3342424 Ki = 237.0 nM 6.62
CHEMBL3342420 Ki = 247.0 nM 6.61
CHEMBL3342413 Ki = 248.0 nM 6.61