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Assay Detail

CHEMBL879999

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Binding
Inhibitory activity was determined against Leukotriene A4 hydrolase
ChEMBL ↗
71
Total Activities
71
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Leukotriene A-4 hydrolase (CHEMBL4618) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationship studies on 1-[2-(4-Phenylphenoxy)ethyl]pyrrolidine (SC-22716), a potent inhibitor of leukotriene A(4) (LTA(4)) hydrolase.
Penning TD, Chandrakumar NS, Chen BB, Chen HY, Desai BN, Djuric SW, Docter SH, Gasiecki AF, Haack RA, Miyashiro JM, Russell MA, Yu SS, Corley DG, Durley RC, Kilpatrick BF, Parnas BL, Askonas LJ, Gierse JK, Harding EI, Highkin MK, Kachur JF, Kim SH, Krivi GG, Villani-Price D, Pyla EY, Smith WG.
J Med Chem (2000) 43 : 721 -735
PubMed 10691697 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 71 6.80 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL85320 KELATORPHAN — 1 8.30
CHEMBL163478 — — 1 8.22
CHEMBL162432 — — 1 8.18
CHEMBL163178 — — 1 8.15
CHEMBL163807 — — 1 8.05
CHEMBL349189 — — 1 7.96
CHEMBL163822 — — 1 7.77
CHEMBL162788 — — 1 7.70
CHEMBL14608 — — 1 7.58
CHEMBL162180 — — 1 7.57
CHEMBL162424 — — 1 7.52
CHEMBL162347 — — 1 7.52
CHEMBL354233 — — 1 7.48
CHEMBL163567 — — 1 7.44
CHEMBL159263 — — 1 7.43
CHEMBL159808 — — 1 7.40
CHEMBL117132 — — 1 7.37
CHEMBL162156 — — 1 7.33
CHEMBL352092 — — 1 7.28
CHEMBL112522 — — 1 7.26
CHEMBL162624 — — 1 7.22
CHEMBL351648 — — 1 7.22
CHEMBL162835 — — 1 7.17
CHEMBL163209 — — 1 7.16
CHEMBL163037 — — 1 7.16
CHEMBL163266 — — 1 7.12
CHEMBL349672 — — 1 7.11
CHEMBL162607 — — 1 7.11
CHEMBL162161 — — 1 7.10
CHEMBL163265 — — 1 7.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL85320 KELATORPHAN IC50 = 5.0 nM 8.30
CHEMBL163478 — IC50 = 6.0 nM 8.22
CHEMBL162432 — IC50 = 6.6 nM 8.18
CHEMBL163178 — IC50 = 7.0 nM 8.15
CHEMBL163807 — IC50 = 9.0 nM 8.05
CHEMBL349189 — IC50 = 11.0 nM 7.96
CHEMBL163822 — IC50 = 17.0 nM 7.77
CHEMBL162788 — IC50 = 20.0 nM 7.70
CHEMBL14608 — IC50 = 26.0 nM 7.58
CHEMBL162180 — IC50 = 27.0 nM 7.57
CHEMBL162424 — IC50 = 30.0 nM 7.52
CHEMBL162347 — IC50 = 30.0 nM 7.52
CHEMBL354233 — IC50 = 33.0 nM 7.48
CHEMBL163567 — IC50 = 36.0 nM 7.44
CHEMBL159263 — IC50 = 37.0 nM 7.43
CHEMBL159808 — IC50 = 40.0 nM 7.40
CHEMBL117132 — IC50 = 43.0 nM 7.37
CHEMBL162156 — IC50 = 47.0 nM 7.33
CHEMBL352092 — IC50 = 53.0 nM 7.28
CHEMBL112522 — IC50 = 55.0 nM 7.26
CHEMBL162624 — IC50 = 60.0 nM 7.22
CHEMBL351648 — IC50 = 60.0 nM 7.22
CHEMBL162835 — IC50 = 67.0 nM 7.17
CHEMBL163209 — IC50 = 69.0 nM 7.16
CHEMBL163037 — IC50 = 70.0 nM 7.16
CHEMBL163266 — IC50 = 75.0 nM 7.12
CHEMBL162607 — IC50 = 77.0 nM 7.11
CHEMBL349672 — IC50 = 77.0 nM 7.11
CHEMBL162161 — IC50 = 80.0 nM 7.10
CHEMBL163265 — IC50 = 87.0 nM 7.06
CHEMBL350586 — IC50 = 100.0 nM 7.00
CHEMBL164168 — IC50 = 100.0 nM 7.00
CHEMBL163144 — IC50 = 150.0 nM 6.82
CHEMBL162439 — IC50 = 150.0 nM 6.82
CHEMBL165407 — IC50 = 190.0 nM 6.72
CHEMBL163428 — IC50 = 190.0 nM 6.72
CHEMBL119054 — IC50 = 200.0 nM 6.70
CHEMBL351207 — IC50 = 220.0 nM 6.66
CHEMBL350833 — IC50 = 230.0 nM 6.64
CHEMBL162979 — IC50 = 260.0 nM 6.58
CHEMBL3084969 — IC50 = 370.0 nM 6.43
CHEMBL26424 TESMILIFENE IC50 = 400.0 nM 6.40
CHEMBL162865 — IC50 = 480.0 nM 6.32
CHEMBL162322 — IC50 = 590.0 nM 6.23
CHEMBL349368 — IC50 = 630.0 nM 6.20
CHEMBL162668 — IC50 = 670.0 nM 6.17
CHEMBL163179 — IC50 = 700.0 nM 6.16
CHEMBL348927 — IC50 = 700.0 nM 6.16
CHEMBL162158 — IC50 = 840.0 nM 6.08
CHEMBL164353 — IC50 = 900.0 nM 6.05