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. Author manuscript; available in PMC: 2019 Aug 23.
Published in final edited form as: Reprod Toxicol. 2017 May 17;70:82–96. doi: 10.1016/j.reprotox.2017.05.005

Table 3.

ToxCast in vitro HTS Assay Data: 25th Percentile AC50 Values

(A) 5HPP-33
Assay Endpoint1 Description Endpoint Classification AC50 (μM)
ATG_ERa_TRANS_up Increase in ER alpha transactivation in HepG2 cells estrogen receptor alpha 0.168
TOX21_ERa_LUC_BG1_Agonist Agonism against ER 1 in BG1 cells estrogen receptor alpha 0.196
ATG_PXR_TRANS_up Increase in PXR transactivation in HepG2 cells xenosensor 0.263
OT_ERa_EREGFP_0480 Increase in ERa fluorescent protein induction in HeLa cells estrogen receptor alpha 0.306
OT_ERa_EREGFP_0120 Increase in ERa fluorescent protein induction in HeLa cells estrogen receptor alpha 0.317
ACEA_T47D_80hr_Positive Effect on cell growth kinetics in T47D cells Cell growth regulation 0.448
TOX21_ERa_BLA_Agonist_ratio Induction of ERa beta lactamase in HEK293T cells estrogen receptor alpha 0.520
NVS_ENZ_hPI3Ka Inhibition of human PI3K enzyme activity (cell-free) Cell growth regulation 0.572
NVS_NR_mERa Cell-free binding to the mouse estrogen receptor alpha mouse estrogen receptor liganding 0.980
Tox21_p53_BLA_ratio2 Activation of p53 signaling pathway in HCT116 cells cell cycle checkpoint 1.036
NVS_NR_bER Cell-free binding to the bovine estrogen receptor alpha bovine estrogen receptor liganding 1.062
NVS_NR_hER Cell-free binding to the human estrogen receptor alpha human estrogen receptor liganding 1.337
OT_ER_ERbERb_0480 Increase in ERb fluorescent protein induction in HeLa cells estrogen receptor 1.396
OT_ER_ERaERb_0480 Increase in ERa fluorescent protein induction in HEK293T cells estrogen receptor 1.618
TOX21_MMP_ratio_down Decreased membrane potential in HEPG2 cells mitochondrial depolarization 2.518
NVS_ENZ_oCOX1 Cell-free enzymatic activity to sheep prostaglandin-endoperoxide synthase 1 cyclooxygenase-1 activity 2.770
BSK_3C_Proliferation_down Decrease in proliferation in umbilical vein endothelial cells Cell growth regulation 2.900
APR_HepG2_p53Act_72h_up Activation of p53 in HepG2 cells cell cycle checkpoint 3.074
BSK_3C_Vis_down Decrease in visual activity in umbilical vein endothelial cells Cellular health 3.202
ATG_ERE_CIS_up Increase in ERS1 activation in HepG2 cells ER steroid hormone activity 3.625
APR_HepG2_MitoticArrest_24h_up Increase in mitochondrial arrest at 24h in HepG2 cells Cell growth regulation 3.760
BSK_4H_MCP1_up CCL2 upregulation in vascular umbilical vein endothelial cells Inflammatory cytokine signals 3.765
ATG_PXRE_CIS_up Increase in PXR activation in HepG2 cells xenosesnor 4.064
OT_ER_ERaERa_0480 Agonism against ER 1 in HEK293T cells ER steroid hormone activity 4.196
NVS_NR_hPXR Inhibition of human PXR binding (cell-free) xenosensor 4.256
CEETOX_H295R_TESTO_dn Decreased catalytic activity of testosterone in H295R cells steroidogenesis 4.377
ATG_DR5_CIS_up Increase in RAR cis-activation in HepG2 cells retinoid signaling 4.386
NVS_ADME_hCYP2C9 Cell-free enzyme activity at human Cyp2C9 Detoxification/ metabolism 4.403
NHEERL_ZF_144hpf_TERATOSCORE_up Increase in TERATOSCORE in zebrafish at 144hpf Abnormal embryo development 4.440
BSK_3C_IL8_up Increase in IL-8 protein levels in umbilical vein endothelial cells Inflammatory cytokine signals 4.528
BSK_LPS_IL8_up CXCL8 downregulation in vascular umbilical vein endothelial cell/peripheral blood mononuclear cell cocultures Inflammatory cytokine signals 4.687
APR_HepG2_MitoMass_72h_up Increase in mitochondrial mass in HepG2 cells mitochondrial number 4.746
BSK_hDFCGF_TIMP1_up Increase in TIMP metallopeptidase inhibitor protein levels in foreskin fibroblast cells Extracellular matrix remodelling 4.754
NVS_ENZ_oCOX2 Inhibition of sheep COX2 enzymatic activity (cell-free) cyclooxygenase-2 activity 4.911
TOX21_TR_LUC_GH3_Antagonist Antagonism of thyroid hormone receptor alpha and beta in GH3 cells Nuclear receptor activity 5.177
NVS_ADME_hCYP2C19 Inhibition of human CYP2C19 activity (cell-free) Detoxification/ metabolism 5.677
APR_HepG2_CellCycleArrest_24h_dn Decrease in cell cycle arrest at 24h in HepG2 cells Cell growth regulation 5.946
APR_HepG2_CellCycleArrest_72h_dn Decrease in cell cycle arrest at 72h in HepG2 cells Cell growth regulation 6.384
BSK_4H_Pselectin_down Decrease in P-selectin protein levels in umbilical vein endothelial cells Endothelial cell-related signaling 6.740
APR_HepG2_StressKinase_24h_up Increase in stress kinase enzyme activity at 24h in HepG2 cells Cellular stress 7.050
BSK_3C_HLADR_down Decrease in major histocompatibility complex, class II, DR alpha levels in umbilical vein endothelial cells Immune function 7.101
APR_HepG2_MitoticArrest_72h_up Increase in cell cycle arrest in HepG2 cells Cell growth regulation 7.368
BSK_LPS_CD40_down Decrease in CD40 (TNF receptor superfamily member 5) in vascular umbilical vein endothelial cell/peripheral blood mononuclear cell cocultures Immune and inflammatory regulation 7.566
1

Additional assay information downloadable at https://www3.epa.gov/research/COMPTOX/toxcast_assay.html

2

Assay run multiple times (5) with consistent results (AC50 range 1.04–3.18 μM)